BDBM235670 Dexamethasone sodium phosphate
BDBM323654 US10188667, Dexamethasone
dexamethasone (tetramethyl-rhodamine conjugated ) BDBM18703
dexamethasone (1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dihydroxy-14-(2-hydroxyacetyl)-2,13,15-trimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-dien-5-one BDBM18207 US11554172, Compound Dexamethasone dexamethasone (tetramethyl-rhodamine conjugated ) US10869929, Compound Dexamethasone
Carbamyl phosphate BDBM50162819 CHEMBL369105 carbamoyl phosphate carbamic phosphoric monoanhydride monocarbamoyl phosphate aminocarbonyl dihydrogen phosphate carbamoyl dihydrogen phosphate
CYCLODEXTRIN PHOSPHATE BDBM50229336 Cyclodextrin Phosphate
4-Nitrophenyl phosphate disodium salt hexahydrate 4-nitrophenyl phosphate (pNPP) para-nitrophenyl phosphate (pNPP) BDBM13466 disodium (4-nitrophenyl) phosphate
Na2HPO4 disodium monohydrogen phosphate disodium hydrogen phosphate Disodium phosphate disodium acid orthophosphate BDBM50080995 disodium hydrogenphosphate Dibasic sodium phosphate CHEMBL1060
BDBM50422306 TRICIRIBINE PHOSPHATE Triciribine Phosphate Salt Of Tricyclic Nucleoside
Riboflavin 5''-Phosphate BDBM50421345 RIBOFLAVIN 5'-PHOSPHATE E101a
sodium dihydrogen phosphate NaH2PO4 monosodium phosphate CHEMBL1368 BDBM50155534 sodium phosphate, monobasic sodium dihydrogenphosphate sodium phosphate monobasic anhydrous phosphoric acid, monosodium salt
Photrexa Riboflavin 5''-phosphate sodium RIBOFLAVIN 5'-PHOSPHATE SODIUM Phosphated riboflavin Riboflavin sodium phosphate BDBM50523758
BDBM50292724 arabinouridine 3'-phosphate CHEMBL460901 URACIL ARABINOSE-3'-PHOSPHATE
2-amino-ethanol dihydrogen phosphate O-phosphocolamine ethanolamine O-phosphate OPE phosphonoethanolamine monoaminoethyl phosphate colaminphosphoric acid 2-amino-ethanol phosphate PEA colamine phosphate mono(2-aminoethyl) phosphate colamine phosphoric acid 2-aminoethyl dihydrogen phosphate phosphoric acid 2-aminoethyl phenyl ester CHEMBL146972 BDBM50281572 EAP ethanolamine acid phosphate pEtN O-phosphoethanolamine
BDBM241975 Clindamycin phosphate
Homoserine phosphate BDBM92999
p-nitrophenyl phosphate BDBM24514 CHEMBL24231 4-nitrophenyl phosphate 4-nitrophenoxyphosphonic acid
sodium phosphate, tribasic tertiaeres Natriumphosphat(V) tribasic sodium orthophosphate sodium orthophosphate CHEMBL363100 phosphoric acid trisodium salt sodium phosphate tertiary sodium phosphate tribasic sodium phosphate BDBM50155537 Na3PO4 Trinatriumphosphat
4-Methylumbelliferyl phosphate BDBM213237
CHEMBL1756 BDBM50333645 Estramustine phosphate
Estradiol phosphate BDBM50333647 CHEMBL1642763
Phosphate analogue, 6 BDBM84557
Phosphate analogue, 9 BDBM84558
mannose 6-phosphate BDBM50275807
BDBM50118216 pyridoxal 5'-phosphate CHEMBL82202 (4-formyl-5-hydroxy-6-methylpyridin-3-yl)methyl dihydrogen phosphate pyridoxal 5'-(dihydrogen phosphate)
BDBM197174 Glucose-6-phosphate (G6P)
BDBM231698 p-Nitrophenyl phosphate (pNPP)
BDBM84559 Phosphate analogue, (s)-14
BDBM84560 Phosphate analogue, (S)-21
para-nitrophenyl phosphate (pNPP) BDBM26100
BDBM50304360 BENZENE-1,2,3,4-TETRAYL TETRAKIS[DIHYDROGEN (PHOSPHATE)] benzene-1,2,3,4-tetrayl tetrakis(hydrogen phosphate) CHEMBL595349
phosphacol p-nitrophenyl diethyl phosphate diethyl p-nitrophenyl phosphate O,O-diethyl O-p-nitrophenyl phosphate CHEMBL23838 diethyl 4-nitrophenyl phosphate diethyl paraoxon paraoxon BDBM50240416 ethyl paraoxon phosphoric acid diethyl 4-nitrophenyl ester
2S,3R-dihydroxybutyramide 4-phosphate BDBM50153711
CHEBI:63036 BDBM50004328 POTASSIUM PHOSPHATE, MONOBASIC
CHEMBL186043 BDBM50155535 Carbamoyl phosphate; di sodium
CHLOROQUINE DIPHOSPHATE CHLOROQUINE PHOSPHATE BDBM50411863 ARALEN
Cytidine 2,3-cyclic phosphate, 6 BDBM31909
Fragment 1 Phosphate phosphoric acid BDBM14671
RUXOLITINIB PHOSPHATE BDBM50391992 INCB018424 SALT Jakafi
4-{hydroxy[(phosphonooxy)acetyl]amino}butyl dihydrogen phosphate N-(4-hydroxybutyl)-glycolohydroxamicacid bis-phosphate CHEMBL1236228 BDBM50330433
BDBM16190 [3-(2-cyanoacetyl)phenyl] diethyl phosphate 3-(2-Cyanoacetyl)phenyl Diethyl Phosphate beta-ketonitrile 5h
DDVP CHEMBL167911 2,2-Dichloroethenyl dimethyl phosphate Dimethyl-2,2-dichlorovinyl phosphate Phosphoric acid, 2,2-dichloroethenyl dimethyl ester Dimethyl 2,2-dichlorovinyl phosphate BDBM50286926 Phosphoric acid, 2,2-dichlorovinyl dimethyl ester
AMP adenosine 5'-phosphate group [5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl phosphate BDBM92538
US10676467, Compound S1P (2S,3R,4E)-2-amino-4-octadecene-1,3-diol 1-(dihydrogen phosphate) (2S,3R,4E)-2-amino-3-hydroxyoctadec-4-en-1-yl dihydrogen phosphate BDBM50158348 CHEMBL225155 sphingosine-1-phosphate US11584726, Example S1P sphingosine 1-phosphate
1-deoxy-L-ribulose 5-phosphate BDBM50153712
4S-hydroxypentan-2-one 5-phosphate BDBM50153714
BDBM50153710 3S-hydroxypentan-2-one 5-phosphate
BDBM92531 DiFMUP (6,8-Difluoro-4-methylumbelliferyl phosphate)
CHEMBL1230617 8-Bromo-Adenosine Mono Phosphate BDBM50222467
CHEMBL1275924 Phenyl-N-(4-aminopiperidine)phosphate BDBM50330376
CHEMBL1775011 8-phenyl-Adenosine Mono Phosphate BDBM50343897
1-(2-bromo-4-chloro-phenyl)sulfonylpiperidine 1-[(2-bromo-4-chlorophenyl)sulfonyl]piperidine MLS000028544 BDBM44576 DEXAMETHASONE 21-ACETATE MLS000060983 SMR000058327 1-(2-bromo-4-chlorophenyl)sulfonylpiperidine DEXAMETHASONE ACETATE cid_772156 SMR000069748 cid_236702 1-(2-bromanyl-4-chloranyl-phenyl)sulfonylpiperidine
sphingosine-1-phosphate, 33P labeled {[(4Z)-2-amino-3-hydroxyoctadec-4-en-1-yl]oxy}phosphonic acid S1P [32P]S1P [33P]S1P BDBM22202 sphingosine-1-phosphate sphingosine-1-phosphate, 32P labeled
2-(methylsulfonamido)-2-oxoethyl dihydrogen phosphate BDBM50175714 CHEMBL370845
BDBM50300123 2-(4-Formylphenoxy)ethyl dimethyl phosphate CHEMBL574442
BDBM50300582 CHEMBL573979 Dibutyl 2,2,2-trifluoro-1-phenylethyl phosphate
CHEBI:83326 TEDIZOLID PHOSPHATE BDBM50017198 TR-701-FA
CHEMBL575281 Dimethyl 2,2,2-trifluoro-1-phenylethyl phosphate BDBM50300580
CHEMBL575301 Diethyl 2,2,2-trifluoro-1-phenylethyl phosphate BDBM50300581
CHEMBL606220 CHEMBL1230617 BDBM50367001 8-Bromo-Adenosine Mono Phosphate
Fludarabine Phosphate Fludarabine Fludara BDBM50248004 CHEBI:63599 Oforta
Hexadecyl[2-(N-Methylpiperidinio)ethyl]phosphate hexadecyl 2-(1-methylpiperidinium-1-yl)ethyl phosphate BDBM50051816 (N-methylpiperidino)ethanol hexadecyl phosphonate CHEMBL89618
1,2-dideoxy-L-threo-3-hexulose 6-phosphate BDBM50153715
2-Methoxy-4-(nonanamidomethyl)phenyl dihydrogen phosphate (3b) BDBM165191
BDBM165193 4-(Nonanamidomethyl)-1,2-phenylene bis(dihydrogen phosphate) (6b)
BDBM50175712 CHEMBL199843 2-oxo-2-(phenylsulfonamido)ethyl dihydrogen phosphate
CHEMBL202243 BDBM50176400 (R)-2,3-bis(octyloxy)propyl dihydrogen phosphate
Etopophos preservative free Etoposide Phosphate BMY-40481 Etopophos BDBM50247889
TCP CAS_78-30-8 BDBM82063 TRI-O-CRESYL PHOSPHATE
beta-nicotinamide adenine dinucleotide phosphate, oxidized form NADP+ BDBM11939
Di-Sodium salt of Phosphoric acid mono-{2-methoxy-5-[2-(3,4,5-trimethoxy-phenyl)-vinyl]-phenyl} ester Disodium Phosphoric acid mono-{2-methoxy-5-[2-(3,4,5-trimethoxy-phenyl)-vinyl]-phenyl} ester combretastatin A-4 sodium phosphate BDBM50064259 Phosphoric acid mono-{2-methoxy-5-[(Z)-2-(3,4,5-trimethoxy-phenyl)-vinyl]-phenyl} ester; disodium salt sodium(Z)-2-methoxy-5-(3,4,5-trimethoxystyryl)phenyl phosphate combretastatin A-4 phosphate Combretastatin A4 phosphate disodium 2-methoxy-5-[(Z)-2-(3,4,5-trimethoxyphenyl)vinyl]phenyl phosphate CHEMBL289351 sodium (Z)-5-(3,4,5-trimethoxystyryl)-2-methoxyphenyl phosphate disodium mono(Z)-5-(3,4,5-trimethoxystyryl)-2-methoxyphenyl phosphate
2-[(3-bromophenyl)carbamoyl]-5-chlorophenyl diethyl phosphate (20) BDBM150740
2-[(4-bromophenyl)carbamoyl]-5-chlorophenyl diethyl phosphate (23) BDBM150743
BDBM50032981 Phosphate analogue, 8 (3-Amino-propyl)-phosphonic acid CHEMBL286077
BDBM50247086 Chlorphrifos oxon diethyl 3,5,6-trichloropyridin-2-yl phosphate CHEMBL444970
CHEMBL1235276 BDBM50330438 3-{hydroxy[(phosphonooxy)acetyl]amino}propyl dihydrogen phosphate
Phosphoglycolohydroxamic Acid BDBM50167777 2-(hydroxyamino)-2-oxoethyl dihydrogen phosphate CHEMBL371668
2-amino-4,5-dihydronaphtho[1,2-d][1,3]thiazol-8-yl dihydrogen phosphate 2-amino-4,5-dihydronaphtho[1,2-d]thiazol-8-yl dihydrogen phosphate BDBM50302495 CHEMBL565809
cori ester glucose-1-phosphate alpha-glucose-1-phosphate BDBM23188 {[(2R,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy}phosphonic acid
2-(hydroxy(3-hydroxypropyl)amino)-2-oxoethyl hydrogen phosphate BDBM50330436 CHEMBL1276292
2-Methoxy-4-((8-methylnonanamido)methyl)phenyl dihydrogen phosphate (3a) BDBM165190
3-Nitro-1-(beta-D-ribofuranosyl)pyrrole 5'-phosphate BDBM50247810 CHEMBL538120
4-Nitro-1-(-beta-D-ribofuranosyl)pyrazole 5'-phosphate BDBM50247822 CHEMBL538121
5-chloro-2-[(3-chlorophenyl)carbamoyl]phenyl diethyl phosphate (19) BDBM150739
5-chloro-2-[(3-fluorophenyl)carbamoyl]phenyl diethyl phosphate (21) BDBM150741
5-chloro-2-[(4-fluorophenyl)carbamoyl]phenyl diethyl phosphate (22) BDBM150742
5-formyl-6-hydroxy-2-naphthyl di-sodium phosphate BDBM50183272 CHEMBL382634
BDBM150744 5-chloro-2-[(4-chlorophenyl)carbamoyl]phenyl diethyl phosphate (24)
BDBM150745 5-chloro-2-[(3,4-dichlorophenyl)carbamoyl]phenyl diethyl phosphate (25)
BDBM165192 4-((8-Methylnonanamido)methyl)-1,2-phenylene bis(dihydrogen phosphate) (6a)
BDBM50247808 CHEMBL538119 3-Nitro-1-(beta-D-ribofuranosyl)imidazole 5'-phosphate
[5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl hydrogen phosphate;triethylazanium SMR000718807 [5-(6-aminopurin-9-yl)-3,4-dihydroxy-2-oxolanyl]methyl hydrogen phosphate;triethylammonium (5-adenin-9-yl-3,4-dihydroxy-tetrahydrofuran-2-yl)methyl hydrogen phosphate;triethylammonium BDBM61258 cid_16396156 MLS001306424 [5-(6-aminopurin-9-yl)-3,4-bis(oxidanyl)oxolan-2-yl]methyl hydrogen phosphate;triethylazanium
(R)-2-amino-3-(4-octylphenylamino)-3-oxopropyl dihydrogen phosphate CHEMBL227371 BDBM50198840
2-formylphenoxyphosphonic acid BDBM14680 2-formylphenyl dihydrogen phosphate RU78262 CHEMBL286678 Fragment 10
2-hydrazinyl-2-oxoethyl hydrogen phosphate BDBM50167772 Phosphoric acid monohydrazinocarbonylmethyl ester CHEMBL195520
5-Amino-1-(beta-D-ribofuranosyl)-4-nitropyrazole 5'-phosphate CHEMBL554752 BDBM50247824
5-Amino-1-(beta-D-ribofuranosyl)pyrazole-4-carboxylate 5'-phosphate BDBM50247823
5-chloro-2-{[3-(trifluoromethyl)phenyl]carbamoyl}phenyl diethyl phosphate (26) BDBM150746
5-chloro-2-{[4-(trifluoromethyl)phenyl]carbamoyl}phenyl diethyl phosphate (27) BDBM150747
BDBM50198833 CHEMBL228102 (R)-2-amino-3-(3-octylphenylamino)-3-oxopropyl dihydrogen phosphate
BDBM50247809 5-Amino-1-(beta-D-ribofuranosyl)imidazole-4-carboxaldehyde 5'-phosphate
BDBM50312665 Sodium 2-(2-Fluorophenyl)-6,7-methylenedioxyquinolin-4-yl hydrogen phosphate CHEMBL1088572
BDBM50343853 2-(2-(Benzylamino)-6-nitroquinazolin-4-ylamino)ethyl dihydrogen phosphate CHEMBL1774786
CHEMBL1765479 BDBM50342010 5'-phospho-2'-deoxyuridine-3'-pyrophosphate(P'->5')adenosine3'-phosphate
(S)-2-amino-4-(4-(heptyloxy)phenyl)-2-methylbutyl dihydrogen phosphate BDBM50313499 CHEMBL1084929
2-(2-Oxo-1,2-dihydrobenzo[cd]indole-6-sulfonamido)ethyldihydrogen phosphate BDBM50316579 CHEMBL1095991
2-amino-4,5-dihydronaphtho[1,2-d]thiazol-7-yl dihydrogen phosphate CHEMBL566049 BDBM50302494
2-amino-4,5-dihydronaphtho[1,2-d]thiazol-9-yl dihydrogen phosphate BDBM50302496 CHEMBL576125
2-amino-8H-indeno[1,2-d]thiazol-4-yl dihydrogen phosphate CHEMBL578134 BDBM50302493
2-amino-8H-indeno[1,2-d]thiazol-5-yl dihydrogen phosphate BDBM50302492 CHEMBL568771
2-amino-8H-indeno[1,2-d]thiazol-6-yl dihydrogen phosphate BDBM50302491 CHEMBL566670
3-(4,5,6,7-Tetrabromo-2H-1,2,3-benzotriazol-2-yl)propyl dihydrogen phosphate BDBM50276680 CHEMBL459343
5-Amino-1-(beta-D-ribofuranosyl)-1,2,3-triazole-4-carboxylate 5'-phosphate BDBM50247825
BDBM150734 2‐[(4‐bromophenyl)carbamoyl]‐4‐chlorophenyl diethyl phosphate (14)
BDBM150736 2‐[(3‐bromophenyl)carbamoyl]‐4‐chlorophenyl diethyl phosphate (16)
BDBM50316580 6-(2-oxo-1,2-dihydrobenzo[cd]indole-6-sulfonamido)hexyldihydrogen phosphate CHEMBL1095867
CHEMBL1097477 4-(2-Oxo-1,2-dihydrobenzo[cd]indole-6-sulfonamido)-butyldihydrogen phosphate BDBM50316577
CHEMBL1097478 BDBM50316581 5-(2-Oxo-1,2-dihydrobenzo[cd]indole-6-sulfonamido)-pentyldihydrogen phosphate
CHEMBL455775 BDBM50292713 5'-phospho-2'-deoxyuridine 3-pyrophosphate (P'->5') adenosine 3'-phosphate
CHEMBL88487 Hexadecyl[2-(N-Methylmorpholinio)ethyl]phosphate BDBM50051809 (N-methylmorpholino)ethanol hexadecyl phosphonate
Phosphoric Acid Dimethyl Ester 4-Nitro-Phenyl Ester DIMETHYL 4-NITROPHENYL PHOSPHATE BDBM50487989
(3R,4S,5R)-4,5-dihydroxy-3-phosphonooxycyclohexene-1-carboxylic acid Shikimate-3-phosphate BDBM100283
(benzyloxy)(2-formylphenoxy)phosphinic acid PASBN BDBM14688 benzyl 2-formylphenyl hydrogen phosphate Fragment 18
1-(4-Methoxyphenylsulfonamido)-3-morpholinopropan-2-yl dihydrogen phosphate HEA derivative, 7a BDBM50248217 CHEMBL473552
1D-myo-inositol 1,3,4,5-tetrakis(dihydrogen phosphate) CHEMBL23552 BDBM50075651 1D-myo-inositol 1,3,4,5-tetrakisphosphate
1D-myo-inositol 1,4,5,6-tetrakisphosphate BDBM50075649 CHEMBL282059 1D-myo-inositol 1,4,5,6-tetrakis(dihydrogen phosphate)
1D-myo-inositol 4,5-bisphosphate BDBM50284584 CHEMBL21825 1D-myo-inositol 4,5-bis(dihydrogen phosphate)
2-(6-Nitro-2-(4-phenoxyphenylamino)quinazolin-4-ylamino)ethyl dihydrogen phosphate BDBM50343852 CHEMBL1774785
3-(2-Oxo-1,2-dihydrobenzo[cd]indole-6-sulfonamido)propyl dihydrogen phosphate BDBM50316578 CHEMBL1097476
4‐bromo‐2‐[(3‐fluorophenyl)carbamoyl]phenyl diethyl phosphate (1) BDBM150721
4‐bromo‐2‐[(4‐bromophenyl)carbamoyl]phenyl diethyl phosphate (8) BDBM150728
4‐bromo‐2‐[(4‐chlorophenyl)carbamoyl]phenyl diethyl phosphate (3) BDBM150723
4‐chloro‐2‐[(3‐chlorophenyl)carbamoyl]phenyl diethyl phosphate (10) BDBM150730
4‐chloro‐2‐[(3‐fluorophenyl)carbamoyl]phenyl diethyl phosphate (12) BDBM150732
4‐chloro‐2‐[(4‐chlorophenyl)carbamoyl]phenyl diethyl phosphate (11) BDBM150731
BDBM150722 4‐bromo‐2‐[(3‐chlorophenyl)carbamoyl]phenyl diethyl phosphate (2)
BDBM150724 4‐bromo‐2‐[(3,4‐dichlorophenyl)carbamoyl]phenyl diethyl phosphate (4)
BDBM150727 4‐bromo‐2‐[(3‐bromophenyl)carbamoyl]phenyl diethyl phosphate (7)
BDBM150729 4‐bromo‐2‐[(4‐fluorophenyl)carbamoyl]phenyl diethyl phosphate (9)
BDBM150733 4‐chloro‐2‐[(4‐fluorophenyl)carbamoyl]phenyl diethyl phosphate (13)
BDBM150735 4‐chloro‐2‐[(3,4‐dichlorophenyl)carbamoyl]phenyl diethyl phosphate (15)
BDBM50287679 CHEMBL61555 Sodium; benzyl 3,4,5-trihydroxy-6-methyltetrahydro-2H-thiopyran-2-yl hydrogen phosphate
BDBM50315803 2-amino-4-(2-fluoro-4-pentylphenyl)-2-(hydroxymethyl)butyl dihydrogen phosphate CHEMBL1095889
BDBM50315805 2-amino-4-(4'-butoxybiphenyl-4-yl)-2-(hydroxymethyl)butyl dihydrogen phosphate CHEMBL1096211
HEA derivative, 7b BDBM50248218 CHEMBL473752 1-(4-Fluorophenylsulfonamido)-3-morpholinopropan-2-yl dihydrogen phosphate
4-THIOURIDINE-5'-MONOPHOSPHATE 4-THIOURIDINE-5'-PHOSPHATE BDBM50341895 ((2R,3S,4R,5R)-3,4-dihydroxy-5-(2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)tetrahydrofuran-2-yl)methyl dihydrogen phosphate CHEMBL1230331
dihydrogen phosphate;2-[2-(4-fluorophenyl)sulfanylethyl]pyridin-1-ium BDBM45710 2-[2-(4-Fluoro-phenylsulfanyl)-ethyl]-pyridinium dihydrogen phosphate;2-[2-[(4-fluorophenyl)thio]ethyl]pyridin-1-ium cid_16682387 MLS000767112 SMR000429527
O-phosphoryl-4-hydroxy-N,N-dimethyltryptamine 4-phosphoryloxy-N,N-dimethyltryptamine US11597738, Example 4 BDBM50171269 Indocybin psilocybin 3-[2-(dimethylamino)ethyl]-1H-indol-4-yl dihydrogen phosphate psilocin phosphate ester Psilocybine CHEMBL194378
(2S)-2-amino-3-(phosphonooxy)propanoic acid BDBM17664 CHEMBL284377 L-serine O-phosphate L-SOP
4‐chloro‐2‐{[3‐ (trifluoromethyl)phenyl]carbamoyl}phenyl diethyl phosphate (17) BDBM150737
BDBM150725 4‐bromo‐2‐{[3‐ (trifluoromethyl)phenyl]carbamoyl}phenyl diethyl phosphate (5)
BDBM150726 4‐bromo‐2‐{[4‐ (trifluoromethyl)phenyl]carbamoyl}phenyl diethyl phosphate (6)
BDBM150738 4‐chloro‐2‐{[4‐ (trifluoromethyl)phenyl]carbamoyl}phenyl diethyl phosphate (18)
BDBM50110800 P,P'-Bis {[4-(guanine-9-yl)cyclopent-2-enyl]oxy-methylphosphonyl}phosphate CHEMBL23886
CHEMBL277903 P,P'-Bis {[4-(adenine-9-yl)cyclopent-2-enyl]oxy-methylphosphonyl}phosphate BDBM50110798
CHEMBL475495 (S)-2-amino-2-methyl-3-(4-(octyloxy)phenylamino)-3-oxopropyl dihydrogen phosphate BDBM50277148
PAS219 (cyclohexylmethoxy)(2-formylphenoxy)phosphinic acid BDBM14685 CHEMBL24811 Fragment 15 cyclohexylmethyl 2-formylphenyl hydrogen phosphate
MLS001306420 SMR000718790 [(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-bis(oxidanyl)oxolan-2-yl]methyl dihydrogen phosphate;hydrate cid_6419976 BDBM70140 [(2R,3S,4R,5R)-5-adenin-9-yl-3,4-dihydroxy-tetrahydrofuran-2-yl]methyl dihydrogen phosphate;hydrate [(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl dihydrogen phosphate;hydrate [(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxy-2-oxolanyl]methyl dihydrogen phosphate;hydrate
(1R,3S,4R,6R)-4,5,6-trihydroxy-2-methyl-2,3-bis(phosphonooxy)cyclohexyl dihydrogen phosphate BDBM50075648 CHEMBL281132
(R)-2-amino-2-((R)-6-octyl-1,2,3,4-tetrahydronaphthalen-2-yl)propyl dihydrogen phosphate BDBM50314403 CHEMBL1089004
(S)-2-amino-2-((R)-6-octyl-1,2,3,4-tetrahydronaphthalen-2-yl)propyl dihydrogen phosphate BDBM50314404 CHEMBL1089005
(S)-2-amino-2-((S)-6-octyl-1,2,3,4-tetrahydronaphthalen-2-yl)propyl dihydrogen phosphate CHEMBL1090758 BDBM50314405
(S)-2-amino-3-(4-(4-cyclohexylbutoxy)phenylamino)-2-methyl-3-oxopropyl dihydrogen phosphate BDBM50249153 CHEMBL473562
1,2,3,4-tetrahydroquinolin-8-yl dihydrogen phosphate (1,2,3,4-tetrahydroquinolin-8-yloxy)phosphonic acid Fragment 12 RU79073 BDBM14682
BDBM14681 RU78299 CHEMBL421138 Fragment 11 2,6-diformyl-4-methylphenoxyphosphonic acid 2,6-diformyl-4-methylphenyl dihydrogen phosphate
BDBM50314402 (R)-2-amino-2-((S)-6-octyl-1,2,3,4-tetrahydronaphthalen-2-yl)propyl dihydrogen phosphate CHEMBL1093686
BDBM50315804 2-amino-4-(3-chloro-4'-pentylbiphenyl-4-yl)-2-(hydroxymethyl)butyl dihydrogen phosphate CHEMBL1096210
CHEMBL195976 Phosphoric acid mono-(N-hydroxycarbamimidoylmethyl) ester BDBM50167775 (Z)-2-amino-2-(hydroxyimino)ethyl hydrogen phosphate
CHEMBL25186 RU78300 2-formyl-6-methoxyphenoxyphosphonic acid 2-formyl-6-methoxyphenyl dihydrogen phosphate BDBM14679 Fragment 9
CHEMBL611046 BDBM50304359 (2R,3S,5S,6S)-6-(hydrogen phosphonato)-3,5-dihydroxycyclohexane-1,2,4-triyl tris(hydrogen phosphate)
US10233190, Example 1434 BDBM370515 sodium 1-cyclohexyl-2-(5H-imidazo[5,1- a]isoindol-5-yl)ethyl phosphate
US11046646, Example 14 BDBM506618 (3-amino-1-(4-octylbenzyl)-2-oxopyrrolidin-3-yl)methyl dihydrogen phosphate
6-hydroxy-UMP 1-beta-D-ribofuranosyl(3H)pyrimidine-2,4,6-trione 5'-monophosphate 6-HYDROXYURIDINE-5'-PHOSPHATE 3,4-dihydroxy-5-(6-oxido-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)tetrahydrofuran-2-yl)methyl phosphate BDBM50199178 CHEMBL383923
(2R,3R,4S)-2,3,4-trihydroxy-5-(hydroxyamino)-5-oxopentyl phosphate BDBM50342610 5-PHOSPHO-D-ARABINOHYDROXAMIC ACID CHEMBL1235136
(R)-2-amino-2-(4-(4-(octyloxy)phenyl)-1H-imidazol-2-yl)propyl dihydrogen phosphate BDBM50277186 CHEMBL474689
2,3,4-trihydroxy-5-oxohexane-1,6-diyl bis(dihydrogen phosphate) BDBM50330437 1,6-di-O-phosphono-D-fructose CHEMBL1235112
2-[hydroxy(4-hydroxybutyl)amino]-2-oxoethyl dihydrogen phosphate BDBM50330439 CHEMBL1236227 N-(4-hydroxybutyl)-phospho-glycolohydroxamic acid
2-amino-3-hydroxy-2-((R)-6-octyl-1,2,3,4-tetrahydronaphthalen-2-yl)propyl dihydrogen phosphate CHEMBL1091103 BDBM50314401
BDBM50080321 ZMP [5-(5-amino-4-carbamoyl-1H-imidazol-1-yl)-3,4-dihydroxyoxolan-2-yl]methyl phosphate
BDBM50249114 CHEMBL473156 (S)-2-amino-2-methyl-3-oxo-3-(4-(5-phenylpentyloxy)phenylamino)propyl dihydrogen phosphate
BDBM50249154 CHEMBL473563 (S)-2-amino-3-(4-(biphenyl-4-ylmethoxy)phenylamino)-2-methyl-3-oxopropyl dihydrogen phosphate
BDBM50277149 CHEMBL515921 (S)-2-amino-3-(3-fluoro-4-(octyloxy)phenylamino)-2-methyl-3-oxopropyl dihydrogen phosphate
CHEMBL1683319 5-O-phosphate-1-N-(4'-(4''-methoxyhenyl))-[1',2',3']-triazol-beta-D-ribofuranoside BDBM50338502
CHEMBL514302 BDBM50249113 (S)-2-amino-2-methyl-3-oxo-3-(4-(4-phenylbutoxy)phenylamino)propyl dihydrogen phosphate
CHEMBL515603 (S)-2-amino-3-(4-(biphenyl-4-yloxy)phenylamino)-2-methyl-3-oxopropyl dihydrogen phosphate BDBM50249238
[(2-cyanoquinolin-8-yl)oxy]phosphonic acid RU79072 Fragment 14 BDBM14684 2-cyanoquinolin-8-yl dihydrogen phosphate
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- ChEMBL_728108 (CHEMBL644022) Displacement of radiolabeled Dexamethasone from GR
- ChEBML_123499 Displacement of [3H]dexamethasone from human mineralocorticoid receptor
- ChEBML_159372 Displacement of [3H]dexamethasone from human progesterone receptor
- ChEBML_36109 Displacement of [3H]dexamethasone from human androgen receptor
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- ChEMBL_372312 (CHEMBL686170) Inhibition of fluorescent-labeled Dexamethasone binding to GR
- ChEMBL_437577 (CHEMBL873175) Displacement of radiolabeled Dexamethasone from human GR
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- ChEMBL_479540 (CHEMBL691172) Displacement of radiolabeled Dexamethasone from glucocorticoid receptor
- ChEMBL_71405 (CHEMBL616193) Displacement of [3H]- Dexamethasone from glucocorticoid receptor
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- ChEMBL_305749 (CHEMBL620408) Inhibition of [3H]dexamethasone binding to human glucocorticoid receptor
- ChEMBL_440116 (CHEMBL657651) Displacement of [3H]dexamethasone from human recombinant GR
- ChEMBL_452405 (CHEMBL665908) Displacement of fluorescent labeled Dexamethasone from glucocorticoid receptor
- ChEMBL_466158 (CHEMBL674561) Displacement of [3H]dexamethasone from human recombinant GR
- ChEMBL_558475 (CHEMBL670406) Displacement of fluorescent labelled Dexamethasone from glucocorticoid receptor
- ChEMBL_71383 (CHEMBL616455) Inhibition of [3H]dexamethasone binding to human Glucocorticoid Receptor
- ChEMBL_71413 (CHEMBL616201) Inhibition of [3H]dexamethasone binding to human Glucocorticoid Receptor
- ChEMBL_716755 (CHEMBL635439) Displacement of fluorescent-labelled Dexamethasone from glucocorticoid receptor
- ChEMBL_306249 (CHEMBL621690) Inhibition of human glucocorticoid receptor alpha by displacement of [3H]dexamethasone
- ChEMBL_312728 (CHEMBL626830) Inhibition of glucocorticoid receptor Dexamethasone response in reporter gene assay
- ChEMBL_423016 (CHEMBL638957) Inhibition of tetramethylrhodamine labeled dexamethasone binding to GR by FP assay
- ChEMBL_423018 (CHEMBL636912) Inhibition of tetramethylrhodamine labeled dexamethasone binding to MR by FP assay
- ChEMBL_447639 (CHEMBL659910) Agonist activity at GR by GRE activation assay relative to Dexamethasone
- ChEMBL_701245 (CHEMBL615887) Displacement of radiolabeled Dexamethasone from glucocorticoid receptor expressed in baculovirus
- ChEMBL_71101 (CHEMBL616424) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR)
- ChEMBL_739803 (CHEMBL652954) Displacement of radiolabeled Dexamethasone from glucocorticoid receptor expressed in baculovirus
- ChEBML_71420 Competitive displacement of [3H]dexamethasone from glucocorticoid receptor of rat liver cytosol
- ChEMBL_1292840 Displacement of [3H]-dexamethasone from human glucocorticoid receptor expressed in HEK293 cells
- ChEMBL_1559801 (CHEMBL1018719) Displacement of [3H]dexamethasone from glucocorticoid receptor in human IM9 cells
- ChEMBL_1633608 (CHEMBL1117751) Displacement of [3H]dexamethasone from GR receptor in human IM9 cells
- ChEMBL_1735710 (CHEMBL1693635) Antagonist activity at human GR assessed as reduction in dexamethasone-induced transactivation
- ChEMBL_312773 (CHEMBL625471) Inhibition of dexamethasone-induced glucocorticoid receptor mediated alkaline phosphatase activity
- ChEMBL_447640 (CHEMBL659911) Antagonist activity at GR assessed as inhibition of dexamethasone-induced GRE activation
- ChEMBL_448942 (CHEMBL661656) Displacement of TAMRA labeled Dexamethasone at human glucocorticoid receptor in insect cell
- ChEMBL_448943 (CHEMBL661657) Displacement of TAMRA labeled Dexamethasone at human progesterone receptor in insect cell
- ChEMBL_634771 (CHEMBL644737) Displacement of fluorescent-labeled Dexamethasone from GR by fluorescent polarization assay
- ChEMBL_71395 (CHEMBL616184) Displacement of 10 nM [3H]dexamethasone from human Glucocorticoid receptor
- ChEMBL_71396 (CHEMBL616185) Displacement of 10 nM [3H]dexamethasone from human Glucocorticoid receptor
- ChEMBL_71397 (CHEMBL616186) Binding affinity towards glucocorticoid receptor (GR) by displacing [3H]dexamethasone
- ChEMBL_1700184 (CHEMBL1647177) Antagonist activity at rat glucocorticoid receptor in primary hepatocytes assessed as dexamethasone-induced tyrosine amino transferase activity preincubated for 30 mins followed by dexamethasone addition measured after 20 hrs
- ChEMBL_1700185 (CHEMBL1647178) Antagonist activity at dog glucocorticoid receptor in primary hepatocytes assessed as dexamethasone-induced tyrosine amino transferase activity preincubated for 30 mins followed by dexamethasone addition measured after 20 hrs
- ChEMBL_1700170 (CHEMBL1647163) Antagonist activity at glucocorticoid receptor in human HepG2 cells assessed as inhibition of dexamethasone-induced tyrosine amino transferase activity preincubated for 30 mins followed by dexamethasone addition measured after 20 hrs
- ChEMBL_1700218 (CHEMBL1647319) Antagonist activity at glucocorticoid receptor in human primary hepatocytes assessed as inhibition of dexamethasone-induced tyrosine amino transferase activity preincubated for 30 mins followed by dexamethasone addition measured after 20 hrs
- ChEBML_71100 Binding affinity against human Glucocorticoid receptor (GR) using [3H]dexamethasone as radioligand
- ChEMBL_306508 (CHEMBL624385) Inhibition of dexamethasone-induced glucocorticoid receptor mediated tyrosine aminotransferase in rat hepatocytes
- ChEMBL_457478 (CHEMBL670982) Displacement of [3H]dexamethasone from human glucocorticoid receptor expressed in recombinant baculovirus
- ChEMBL_70937 (CHEMBL616302) Inhibition of Dexamethasone stimulated transcriptional activity in CHO cells expressing glucocorticoid receptor
- ChEMBL_70938 (CHEMBL616117) Inhibition of Dexamethasone stimulated transcriptional activity in CHO cells expressing glucocorticoid receptor
- ChEMBL_839721 (CHEMBL655986) Antagonist activity at glucocorticoid receptor in rat hepatocytes assessed as inhibition of dexamethasone-induced trypsine aminotransferase expression incubated for 30 mins prior to dexamethasone-induction measured after 4 hrs by reporter gene assay
- ChEMBL_1338546 Displacement of TAMRA-labeled dexamethasone from glucocorticoid receptor (unknown origin) by fluorescence polarization assay
- ChEMBL_1446326 (CHEMBL895437) Displacement of tetramethylrhodamine-labeled dexamethasone from PR (unknown origin) by fluorescence polarization assay
- ChEMBL_199711 (CHEMBL713726) Transcriptional repression activity in HEP G2 cells expressing glucocorticoid receptor compared to Dexamethasone
- ChEMBL_306509 (CHEMBL624386) Inhibition of dexamethasone-induced GR-mediated tyrosine amino transferase activity in rat hepatocytes
- ChEMBL_71100 (CHEMBL616423) Binding affinity against human Glucocorticoid receptor (GR) using [3H]dexamethasone as radioligand
- ChEMBL_71400 (CHEMBL873475) Inhibition of Dexamethasone binding to human glucocorticoid receptor expressed in baculovirus SF-12 cells
- ChEMBL_71401 (CHEMBL616189) Displacement of Dexamethasone from human glucocorticoid receptor expressed in baculovirus SF-12 cells
- ChEMBL_726895 (CHEMBL634080) Displacement of [3H]dexamethasone from Sprague-Dawley rat GR by liquid scintillation counting
- ChEMBL_1338548 (CHEMBL867192) Displacement of TAMRA-labeled dexamethasone from mineralocorticoid receptor (unknown origin) by fluorescence polarization assay
- ChEMBL_199710 (CHEMBL713725) Transcriptional repression of IL-1 stimulated IL-6 expression in native cells compared to Dexamethasone
- ChEMBL_466159 (CHEMBL674562) Antagonist activity at GR in SW1353/MMTV5 cells assessed as inhibition of dexamethasone-induced luciferase expression
- ChEMBL_499970 (CHEMBL880197) Displacement of FITC-dexamethasone from human recombinant glucocorticoid receptor alpha by fluorescence polarization assay
- ChEMBL_637924 (CHEMBL650974) Displacement of [3H]dexamethasone from human glucocorticoid receptor after 16 hrs by scintillation counting
- ChEMBL_849777 (CHEMBL662999) Displacement of [3H]-dexamethasone from human full length GR expressed in insect Sf21 cells
- ChEMBL_965461 (CHEMBL682101) Displacement of [3H]Dexamethasone from glucocorticoid receptor in human HeLaS3 cells after 2 hrs
- ChEMBL_556521 (CHEMBL666810) Inhibition of rabbit muscle glycogen phosphorylase assessed as release of phosphate from glucose 1 phosphate
- ChEBML_71109 Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 150-220 nM
- ChEMBL_1277677 Displacement of TAMRA-labeled dexamethasone from glucocorticoid receptor (unknown origin) by fluorescence polarization competitive binding assay
- ChEMBL_1499884 (CHEMBL976216) Displacement of [3H]-dexamethasone from cytosolic fraction of human recombinant glucocorticoid receptor by scintillation counting analysis
- ChEMBL_1620823 (CHEMBL1111272) Displacement of [3H]dexamethasone from human GR measured after 18 hrs by scintillation counting method
- ChEMBL_1864065 (CHEMBL2174813) Displacement of [3H]dexamethasone from recombinant human GR after 360 mins by scintillation counting analysis
- ChEMBL_873662 (CHEMBL681869) Displacement of [3H]dexamethasone from human glucocorticoid receptor overexpressed in HEK293 cells by microbeta counting assay
- ChEMBL_977683 (CHEMBL689861) Displacement of [3H]-Dexamethasone human GR expressed in 293 cells after 16 hrs by scintillation counting
- ChEMBL_1558648 (CHEMBL960686) Inhibition of rabbit muscle glycogen phosphorylase-a assessed as formation of inorganic phosphate from glucose-1-phosphate by colorimetry
- ChEMBL_1827551 (CHEMBL2051579) Displacement of [3H]dexamethasone from GR in human IM9 cells after 6 hrs by scintillation counting method
- ChEMBL_424794 (CHEMBL875669) Activity at GR expressed in CHO cells assessed as decrease in dexamethasone-stimulated alkaline phosphatase production by GRAF assay
- ChEMBL_71102 (CHEMBL616425) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 10-12 nM
- ChEMBL_71103 (CHEMBL616426) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 106-131 nM
- ChEMBL_71104 (CHEMBL616427) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 1273-2947 nM
- ChEMBL_71105 (CHEMBL616428) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 13-26 nM
- ChEMBL_71106 (CHEMBL616290) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 133-161 nM
- ChEMBL_71107 (CHEMBL616052) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 1382-1049 nM
- ChEMBL_71108 (CHEMBL616053) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 1428-1433 nM
- ChEMBL_71109 (CHEMBL616054) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 150-220 nM
- ChEMBL_71110 (CHEMBL616055) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 159-161 nM
- ChEMBL_71111 (CHEMBL616056) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 17-21 nM
- ChEMBL_71112 (CHEMBL616057) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 2-2 nM
- ChEMBL_71113 (CHEMBL616058) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 215-217 nM
- ChEMBL_71114 (CHEMBL616059) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 23-33 nM
- ChEMBL_71115 (CHEMBL616060) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 26-67 nM
- ChEMBL_71116 (CHEMBL616061) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 28-34 nM
- ChEMBL_71117 (CHEMBL616062) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 294-554 nM
- ChEMBL_71118 (CHEMBL616063) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 3-3 nM
- ChEMBL_71228 (CHEMBL616180) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 3-4 nM
- ChEMBL_71229 (CHEMBL616181) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 366-578 nM
- ChEMBL_71230 (CHEMBL616182) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 378-814 nM
- ChEMBL_71231 (CHEMBL616183) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 379-840 nM
- ChEMBL_71232 (CHEMBL615874) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 39-94 nM
- ChEMBL_71233 (CHEMBL615875) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 43-50 nM
- ChEMBL_71234 (CHEMBL615876) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 44-53 nM
- ChEMBL_71235 (CHEMBL615877) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 5-6 nM
- ChEMBL_71236 (CHEMBL615878) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 536-560 nM
- ChEMBL_71237 (CHEMBL615879) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 559-1423 nM
- ChEMBL_71238 (CHEMBL615880) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 6-7 nM
- ChEMBL_71239 (CHEMBL615881) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 6-8 nM
- ChEMBL_71240 (CHEMBL615882) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 61-63 nM
- ChEMBL_71241 (CHEMBL615883) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 639-673 nM
- ChEMBL_71242 (CHEMBL615884) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 681-974 nM
- ChEMBL_71243 (CHEMBL615885) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 70-92 nM
- ChEMBL_71244 (CHEMBL615886) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 838-988 nM
- ChEMBL_71245 (CHEMBL615887) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 9-12 nM
- ChEMBL_71246 (CHEMBL615888) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 949-1169 nM
- ChEMBL_772901 (CHEMBL684216) Displacement of [3H]-dexamethasone from human recombinant glucocorticoid receptor after 18 hrs by liquid scintillation counting
- ChEMBL_595113 (CHEMBL707674) Inhibition of rabbit muscle glycogen phosphorylase A assessed as release of phosphate from glucose-1-phosphate after 25 mins
- ChEMBL_620083 (CHEMBL632613) Inhibition of rabbit muscle glycogen phosphorylase assessed as release of phosphate from glucose-1-phosphate after 25 mins
- ChEMBL_372315 (CHEMBL683577) Activity at GR assessed as ability to antagonize dexamethasone-induced MMTV luciferase reporter gene transactivation in human A549 cells
- ChEMBL_372316 (CHEMBL683578) Agonist activity at GR assessed as MMTV-mediated transactivation of renilla luciferase gene in human A549 cells relative to Dexamethasone
- ChEMBL_479545 (CHEMBL691177) Antagonist activity at glucocorticoid receptor assessed as inhibition of dexamethasone-induced glucose response element transcriptional transactivation by luciferase assay
- ChEMBL_71398 (CHEMBL616187) Binding affinity towards human glucocorticoid receptor (GR) was determined using [3H]dexamethasone as radioligand in SF-1 cells
- ChEMBL_728113 (CHEMBL644026) Agonist activity at human GR expressed in NHDF cells assessed as inhibition of IL-6 production by ELISA relative to Dexamethasone
- ChEMBL_89092 (CHEMBL622918) Repression activity of GR ligand with interleukin-6 receptor in native cell assay using Dexamethasone was determined as maximal potency
- ChEMBL_1360672 Non-competitive inhibition of pyridoxine phosphate oxidase (unknown origin) assessed as oxidation of pyridoxol 5'-phosphate by Lineweaver-Burk plot analysis
- ChEMBL_762684 (CHEMBL676088) Inhibition of rabbit muscle glycogen phosphorylase 1a assessed as release of phosphate from glucose-1- phosphate after 20 mins
- ChEMBL_762685 (CHEMBL676089) Inhibition of human liver glycogen phosphorylase 1a assessed as release of phosphate from glucose-1- phosphate after 20 mins
- ChEMBL_1460187 (CHEMBL926233) Inhibition of rabbit muscle glycogen phosphorylase a assessed as inhibition of release of phosphate from glucose-1-phosphate after 30 mins by spectrophotometry
- ChEMBL_1630551 (CHEMBL1108265) Inhibition of rabbit muscle glycogen phosphorylase-b assessed as release of inorganic phosphate from glucose-1-phosphate in presence of AMP and glycogen
- ChEMBL_99040 (CHEMBL626563) In vitro inhibitory activity against recombinant human liver glycogen phosphorylase a (rHLGPa) catalyzed release of phosphate from glucose-1-phosphate.
- Inhibition Activity Assay Human liver glycogen phsphorylase (HLGP) activity was measured in the direction of glycogen synthesis by the release of phosphate from glucose-1-phosphate.
- ChEMBL_1438889 (CHEMBL889232) Displacement of [3H]-Dexamethasone from glucocorticoid receptor (unknown origin) expressed in 293 cells after 16 hrs by scintillation counting
- ChEMBL_2111613 (CHEMBL717206) Displacement of [3H]dexamethasone from glucocorticoid receptor in human IM-9 cells incubated for 6 hrs by scintillation counting analysis
- ChEMBL_841250 (CHEMBL654376) Displacement of fluorescent labelled SRC1-4 from dexamethasone-GR complex after 2 to 4 hrs by TR-FRET assay
- ChEMBL_886649 (CHEMBL694634) Displacement of [3H]dexamethasone from human recombinant glucocorticoid receptor expressed in baculovirus after 18 hrs by scintillation counting analysis
- ChEMBL_936982 (CHEMBL647754) Displacement of [3H]-dexamethasone human glucocorticoid receptor alpha expressed in 293 MSR cells after 60 mins by scintillation counting
- ChEMBL_447975 (CHEMBL657478) Inhibition of glucose 6 phosphate translocase 1
- ChEMBL_664344 (CHEMBL676075) Inhibition of human recombinant renin in phosphate buffer
- ChEMBL_743385 (CHEMBL653189) Inhibition of mTOR by radiometric phosphate incorporation assay
- ChEMBL_1733215 (CHEMBL1691149) Inhibition of rabbit muscle glycogen phosphorylase-a assessed as release of inorganic phosphate using glucose-1-phosphate as substrate in presence of glycogen by spectrophotometric method
- ChEMBL_1733216 (CHEMBL1691150) Inhibition of human liver glycogen phosphorylase-a assessed as release of inorganic phosphate using glucose-1-phosphate as substrate in presence of glycogen by spectrophotometric method
- ChEMBL_1670145 (CHEMBL1265355) Competitive inhibition of human liver glycogen phosphorylase-a assessed as release of inorganic phosphate using varying levels of glucose-1-phosphate and constant concentration of AMP and glycogen preincubated for 15 mins with AMP and glycogen followed by glucose-1-phosphate addition
- ChEMBL_1275505 Displacement of [3H]dexamethasone from GST-tagged human glucocorticoid receptor ligand binding domain after 4 hrs by liquid scintillation counting
- ChEMBL_1510382 (CHEMBL999548) Displacement of [3H]-dexamethasone from human glucocorticoid receptor expressed in HEK293 cells by scintillation counting based radioligand competition binding assay
- ChEMBL_1755053 (CHEMBL1806109) Displacement of [3H]dexamethasone from human recombinant glucocorticoid receptor expressed in insect cells after 24 hrs by scintillation proximity assay
- ChEMBL_2172765 (CHEMBL780738) Antagonist activity at glucocorticoid receptor in human HeLa cells assessed as reduction in dexamethasone-induced luciferase activity by dual-Glo luciferase assay
- ChEMBL_321122 (CHEMBL638005) Effective concentration against inhibition of Dexamethasone induced glucocorticoid receptor transactivation of mouse mammary tumor virus luciferase gene in HeLa cells
- ChEMBL_448641 (CHEMBL659621) Antagonist activity at glucocorticoid receptor in human A549 cells transfected with MMTV luciferase reporter gene assessed as inhibition of dexamethasone-induced activation
- ChEMBL_452410 (CHEMBL665913) Antagonist activity at glucocorticoid receptor in human A549 cells transfected with MMTV luciferase reporter gene assessed as inhibition of dexamethasone-induced activation
- ChEMBL_457479 (CHEMBL671133) Antagonist activity at human glucocorticoid receptor in SW1353 cells assessed as inhibition of dexamethasone-induced luciferase expression by MMTV5 reporter gene assay
- ChEMBL_663368 (CHEMBL676104) Binding affinity to glucocorticoid receptor expressed in baculovirus-infected insect cells using tetramethylrhodamine labeled Dexamethasone by fluorescence polarization microplate assay
- ChEMBL_663370 (CHEMBL676106) Binding affinity to mineralocorticoid receptor expressed in baculovirus-infected insect cells using tetramethylrhodamine labeled Dexamethasone by fluorescence polarization microplate assay
- ChEMBL_775646 (CHEMBL683295) Displacement of tetramethylrhodamine-labeled Dexamethasone from human recombinant glucocorticoid receptor expressed in baculovirus infected insect cells by fluorescence polarization assay
- ChEMBL_775648 (CHEMBL683297) Displacement of tetramethylrhodamine-labeled Dexamethasone from human recombinant mineralocorticoid receptor expressed in baculovirus infected insect cells by fluorescence polarization assay
- ChEMBL_839719 (CHEMBL655984) Displacement of [3H]dexamethasone from human glucocorticoid receptor expressed in baculovirus infected Sf9 cells after overnight incubation by scintillation counting
- ChEMBL_1619029 (CHEMBL1102071) Inhibition of rabbit skeletal muscle glycogen phosphorylase b assessed as reduction in inorganic phosphate release using glucose-1-phosphate as substrate at pH 6.8
- ChEMBL_753234 (CHEMBL664483) Inhibition of rabbit muscle glycogen phosphorylase A assessed as release of phosphate from glucose-1-phosphate after 25 mins by microplate reader based method
- ChEMBL_797827 (CHEMBL706674) Inhibition of rabbit muscle glycogen phosphorylase a assessed as release of phosphate from glucose-1-phosphate after 25 mins using malachite green staining
- ChEMBL_36028 (CHEMBL627868) Inhibitory activity against Arabinose-5-phosphate isomerase
- ChEMBL_447602 (CHEMBL659813) Inhibition of human PNP in presence of 1 mM phosphate
- ChEMBL_447603 (CHEMBL659814) Inhibition of human PNP in presence of 0.025 mM phosphate
- ChEMBL_447604 (CHEMBL659815) Inhibition of calf PNP in presence of 1 mM phosphate
- ChEMBL_447605 (CHEMBL659816) Inhibition of calf PNP in presence of 0.025 mM phosphate
- ChEMBL_72881 (CHEMBL617784) TInhibition of glyceraldehyde-3-phosphate dehydrogenase in Leishmania mexicana
- ChEMBL_72891 (CHEMBL617609) Inhibition of glyceraldehyde-3-phosphate dehydrogenase in Trypanosoma brucei
- ChEMBL_72903 (CHEMBL617619) Inhibition of Glyceraldehyde-3-phosphate dehydrogenase in human erythrocytes.
- ChEMBL_765397 (CHEMBL674628) Inhibition of PTP1B using p-nitrophenyl phosphate as substrate
- ChEMBL_775058 (CHEMBL688005) Noncompetitive inhibition of GFAT in presence of fructose-6-phosphate
- ChEMBL_882108 (CHEMBL880725) Inhibition of TCPTP by para-nitrophenyl phosphate release assay
- ChEMBL_882109 (CHEMBL694598) Inhibition of PTP1B by para-nitrophenyl phosphate release assay
- ChEMBL_1619018 (CHEMBL1101843) Inhibition of rabbit skeletal muscle glycogen phosphorylase b assessed as inorganic phosphate release using glucose-1-phosphate as substrate by double-reciprocal plot analysis
- ChEMBL_1733214 (CHEMBL1691148) Inhibition of rabbit muscle glycogen phosphorylase-b assessed as release of inorganic phosphate using glucose-1-phosphate as substrate in presence of AMP and glycogen by spectrophotometric method
- ChEBML_1685152 Antagonist activity at human GRalpha expressed in HEK293 cells assessed as inhibition of dexamethasone-induced response after 24 hrs by luciferase reporter gene assay
- ChEMBL_1553954 (CHEMBL965372) Displacement of [3H]-dexamethasone from glucocorticoid receptor (unknown origin) expressed in HEK293 cell lysate incubated overnight by microbeta scintillation counting method
- ChEMBL_1678021 (CHEMBL1281643) Displacement of [3H]-dexamethasone from recombinant human GST-tagged GR ligand binding domain after 4 hrs by liquid scintillation counting
- ChEMBL_1736302 (CHEMBL1693656) Antagonist activity at GR in human PBMC assessed as reduction in dexamethasone-induced GILZ gene expression incubated for 6 hrs by RT-qPCR method
- ChEMBL_1736303 (CHEMBL1693657) Antagonist activity at GR in human PBMC assessed as reduction in dexamethasone-induced FKBP5 gene expression incubated for 6 hrs by RT-qPCR method
- ChEMBL_1736304 (CHEMBL1693658) Antagonist activity at GR in rat PBMC assessed as reduction in dexamethasone-induced GILZ gene expression incubated for 24 hrs by RT-qPCR method
- ChEMBL_1736305 (CHEMBL1693659) Antagonist activity at GR in rat PBMC assessed as reduction in dexamethasone-induced FKBP5 gene expression incubated for 24 hrs by RT-qPCR method
- ChEMBL_1736306 (CHEMBL1693660) Antagonist activity at GR in dog PBMC assessed as reduction in dexamethasone-induced GILZ gene expression incubated for 6 hrs by RT-qPCR method
- ChEMBL_1736307 (CHEMBL1693661) Antagonist activity at GR in dog PBMC assessed as reduction in dexamethasone-induced FKBP5 gene expression incubated for 6 hrs by RT-qPCR method
- ChEMBL_1736312 (CHEMBL1693666) Antagonist activity at GR in human OVCAR5 assessed as reduction in dexamethasone-induced GILZ gene expression incubated for 24 hrs by RT-qPCR method
- ChEMBL_1736313 (CHEMBL1693667) Antagonist activity at GR in human OVCAR5 assessed as reduction in dexamethasone-induced FKBP5 gene expression incubated for 24 hrs by RT-qPCR method
- ChEMBL_474430 (CHEMBL683199) Antagonist activity at human GR ligand binding domain expressed in african green monkey COS7 cells in presence of Dexamethasone by Gal4 hybrid assay
- ChEMBL_839889 (CHEMBL653334) Displacement of [3H]dexamethasone from human glucocorticoid receptor expressed in baculovirus infected Sf9 cells after 16-18 hrs by beta counting
- Fluorescent Coupled Assay The binding affinities to FtsZ were determined by a fluorescent coupled assay for phosphate relase. In this GTPase studies, phosphate liberated during GTP hydrolysis is a substrate of purine nucleoside phosphorylase, which converts 7-methylguanosine to 7-methylguanin and ribose-1-phosphate, resulting in a decrease of fluorescence.
- ChEMBL_2106081 (CHEMBL713228) Inhibition of Fam20C (unknown origin) assessed as reduction in inorganic phosphate release in presence of ATP measured by Malachite green phosphate staining based micro plate reader assay
- ChEMBL_764140 (CHEMBL675304) Competitive inhibition of rabbit muscle glycogen phosphorylase b assessed as inorganic phosphate release using alphaD glucose-1-phosphate as substrate at pH 6.8 by spectrophotometric analysis
- ChEMBL_1736310 (CHEMBL1693664) Antagonist activity at GR in mini pig PBMC assessed as reduction in dexamethasone-induced GILZ gene expression incubated for 24 hrs by RT-qPCR method
- ChEMBL_1736311 (CHEMBL1693665) Antagonist activity at GR in mini pig PBMC assessed as reduction in dexamethasone-induced FKBP5 gene expression incubated for 24 hrs by RT-qPCR method
- ChEMBL_702551 (CHEMBL617102) Modulation of glucocorticoid receptor in human SKGT4 cells assessed as receptor translocation from cytoplasm to nucleus after 4 hrs by Hoechst staining relative to Dexamethasone
- ChEMBL_1455461 (CHEMBL886237) Stimulation of ATPase activity of human MRP2 assessed as inorganic phosphate
- ChEMBL_1455462 (CHEMBL886238) Inhibition of ATPase activity of human MRP2 assessed as inorganic phosphate
- ChEMBL_1455463 (CHEMBL886239) Stimulation of ATPase activity of rat Mrp2 assessed as inorganic phosphate
- ChEMBL_1455464 (CHEMBL886241) Inhibition of ATPase activity of rat Mrp2 assessed as inorganic phosphate
- ChEMBL_302548 (CHEMBL617100) Binding affinity against rabbit muscle triose-phosphate isomerase
- ChEMBL_305228 (CHEMBL623568) Inhibitory concentration against rabbit muscle triose-phosphate isomerase
- ChEMBL_555945 (CHEMBL660600) Activity at human GnRH receptor by inositol phosphate functional assay
- ChEMBL_775079 (CHEMBL686613) Inhibition of GFAT using N-acetylglucosamine 6-phosphate as substrate
- ChEMBL_835427 (CHEMBL643601) Agonist activity at mouse GPR142 assessed as inositol phosphate accumulation
- ChEMBL_882103 (CHEMBL694433) Competitive inhibition of PTP1B by para-nitrophenyl phosphate release assay
- Inhibition Assay Inhibition assay using glucose-1-phosphate thymidylyltransferase (RmlA).
- Inhibition Assay Inhibition assay using sphingosine-1-phosphate receptor 3.
- ChEMBL_1649508 (CHEMBL1219206) Inhibition of rat muscle glycogen phosphorylase A assessed as release of inorganic phosphate from glucose-1- phosphate in presence of glycogen after 30 mins by malachite green based assay
- ChEMBL_907777 (CHEMBL624016) Inhibition of Escherichia coli imidazoleglycerol phosphate dehydratase using imidazole glycerol phosphate as substrate incubated for 30 min prior to substrate addition measured for 16 min by spectrophotometric analysis
- ChEMBL_1736254 (CHEMBL1693398) Antagonist activity at human GR expressed in CHO-K1 cells assessed as reduction in dexamethasone-induced response incubated for 20 hrs by luciferase reporter gene assay
- ChEMBL_802422 (CHEMBL617258) Antagonist activity at glucocorticoid receptor in human A549 cells assessed as inhibition of dexamethasone-induced transcription at GRE after 24 hrs by luciferase reporter gene assay
- ChEMBL_839891 (CHEMBL653335) Antagonist activity at glucocorticoid receptor in rat H4IIE cells assessed as inhibition of dexamethasone-induced trypsine aminotransferase expression after 24 hrs by reporter gene assay
- ChEMBL_873649 (CHEMBL681857) Displacement of TAMRA-labeled Dexamethasone from human mineralocorticoid receptor expressed in baculovirus infected insect cell lysate after 60 mins by fluorescence polarization assay
- ChEMBL_886648 (CHEMBL694633) Antagonist activity at glucocorticoid receptor in human SW1353 cells assessed as inhibition of dexamethasone-induced luciferase expression after 16 hrs by MMTV5 reporter gene assay
- ChEMBL_1878663 (CHEMBL2182487) Inhibition of human recombinant CYP1B1 using 7-ethoxyresorufin as substrate in presence of glucose-6-phosphate, glucose-6-phosphate dehydrogenase and NADPH-generating system incubated for 35 mins by fluorometry
- ChEMBL_1878664 (CHEMBL2182488) Inhibition of human recombinant CYP1A1 using 7-ethoxyresorufin as substrate in presence of glucose-6-phosphate, glucose-6-phosphate dehydrogenase and NADPH-generating system incubated for 15 mins by fluorometry
- ChEMBL_1878665 (CHEMBL2182489) Inhibition of human recombinant CYP1A2 using 7-ethoxyresorufin as substrate in presence of glucose-6-phosphate, glucose-6-phosphate dehydrogenase and NADPH-generating system incubated for 50 mins by fluorometry
- ChEMBL_506139 (CHEMBL884005) Inhibition of Mycobacterium tuberculosis DXR assessed as NADPH-dependent conversion of 1-deoxy-D-xylulose 5-phosphate to 2-C-methyl-D-erythritol 4-phosphate by spectrophotometric method
- ChEBML_158626 Inhibition of human prostatic acid phosphatase was determined as inhibition of the hydrolysis of tyrosine phosphate
- ChEBML_52541 Inhibition of 2-C-methyl-d-erythritol-4-phosphate cytidyltransferase (YgbP)
- ChEBML_69909 Inhibitory concentration against Trypanosoma brucei glyceraldehyde-3-phosphate dehydrogenase (GAPDH)
- ChEBML_71454 Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
- ChEBML_72905 Compound was tested for the inhibition of Leishmania mexicana GAPDH(glyceraldehyde-3-phosphate dehydrogenase)
- ChEMBL_1286129 Competitive inhibition of PFKFB3 (unknown origin) using fructose 6-phosphate as substrate
- ChEMBL_1581173 (CHEMBL1058087) Inhibition of recombinant human PTP1B assessed as hydrolysis of p-nitrophenyl phosphate
- ChEMBL_162205 (CHEMBL672249) Binding affinity against phosphate binding site of Purine nucleoside Phosphorylase
- ChEMBL_1888918 Inhibition of Mycobacterium tuberculosis H37Ra PTPB using p-nitrophenyl phosphate as substrate
- ChEMBL_303122 (CHEMBL617965) Inhibitory activity against Escherichia coli deoxyxylulose 5-phosphate reductoisomerase
- ChEMBL_466588 (CHEMBL680019) Displacement of pentamannosyl phosphate bovine serum albumin from M6P/IGF2R
- ChEMBL_499713 (CHEMBL713728) Displacement of [33P]sphingosine-1-phosphate from human S1P1 receptor
- ChEMBL_499714 (CHEMBL877241) Displacement of [33P]sphingosine-1-phosphate from human S1P3 receptor
- ChEMBL_499715 (CHEMBL713729) Displacement of [33P]sphingosine-1-phosphate from human S1P4 receptor
- ChEMBL_499716 (CHEMBL713730) Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
- ChEMBL_519984 (CHEMBL634982) Inhibition of sphingosine-1-phosphate lyase in mouse spleen by scintillation counting
- ChEMBL_540418 (CHEMBL652633) Displacement of [33P]sphingosine-1-phosphate from human S1P1 receptor
- ChEMBL_540419 (CHEMBL652634) Displacement of [33P]sphingosine-1-phosphate from human S1P3 receptor
- ChEMBL_540420 (CHEMBL652635) Displacement of [33P]sphingosine-1-phosphate from human S1P4 receptor
- ChEMBL_540421 (CHEMBL652636) Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor
- ChEMBL_555946 (CHEMBL660601) Activity at rhesus monkey GnRH receptor by inositol phosphate functional assay
- ChEMBL_606269 (CHEMBL623429) Agonist activity against 5HT2B receptor assessed as inositol phosphate accumulation
- ChEMBL_70744 (CHEMBL615849) Inhibition of rat brain farnesyltransferase in 30 mM potassium phosphate buffer
- ChEMBL_72894 (CHEMBL617612) Inhibitory concentration of compound against glyceraldehyde-3-phosphate dehydrogenase was determined
- ChEMBL_72896 (CHEMBL617614) Inhibitory activity was measured for Glyceraldehyde-3-phosphate dehydrogenase in Trypanosoma brucei
- ChEMBL_72898 (CHEMBL858114) Inhibitory activity was measured for Glyceraldehyde-3-phosphate dehydrogenase in Trypanosoma cruzi.
- ChEMBL_72900 (CHEMBL617617) Inhibitory activity was measured for Glyceraldehyde-3-phosphate dehydrogenase in human(erythrocytes)
- ChEMBL_741887 (CHEMBL655517) Inhibition of Itk after 40 mins by radiometric phosphate incorporation assay
- ChEMBL_743384 (CHEMBL653188) Inhibition of DNAPK after 2 hrs by radiometric phosphate incorporation assay
- ChEMBL_986855 (CHEMBL695027) Inhibition of PTP1B (unknown origin) using p-nitrophenyl phosphate as substrate
- ChEMBL_1295697 Competitive binding affinity to mineralocorticoid receptor (unknown origin) expressed in baculovirus-infected cell system after 1 hr by fluorescence polarization assay in presence of tetramethylrhodamine-labeled dexamethasone
- ChEMBL_1295699 Competitive binding affinity to glucocorticoid receptor (unknown origin) expressed in baculovirus-infected cell system after 1 hr by fluorescence polarization assay in presence of tetramethylrhodamine-labeled dexamethasone
- ChEMBL_1658415 (CHEMBL1247286) Displacement of TAMRA-labeled dexamethasone from full-length human mineralocorticoid receptor expressed in baculovirus infected insect cells after 60 mins by fluorescence polarization assay
- ChEMBL_1735696 (CHEMBL1693621) Antagonist activity at human CMX-GRalpha expressed in HEK293 cells assessed as reduction in dexamethasone-induced transactivation activity after 24 hrs by luciferase reporter gene assay
- ChEMBL_839720 (CHEMBL655985) Antagonist activity at human glucocorticoid receptor expressed in GRAF cells assessed as inhibition of dexamethasone-induced alkaline phosphatase expression after 48 hrs by reporter gene assay
- ChEMBL_839890 (CHEMBL856075) Antagonist activity at human glucocorticoid receptor expressed in CHOK1 cells assessed as inhibition of dexamethasone-induced alkaline phosphatase expression after 46 hrs by reporter gene assay
- ChEMBL_1632373 (CHEMBL1115578) Inhibition of PI3Kbeta in HUVEC assessed as reduction in sphingosine-1-phosphate stimulated akt phosphorylation at Ser473 residue preincubated for 15 mins followed by sphingosine-1-phosphate stimulation for 5 mins by HTRF assay
- ChEMBL_604866 (CHEMBL618293) Inhibition of Escherichia coli type I phosphomannose isomerase assessed as D-mannose 6-phosphate to D-fructose 6-phosphate isomerization at pH 7.1 by PGI/G6PDH coupled enzyme spectrophotometric assay
- ChEMBL_604867 (CHEMBL618294) Inhibition of Saccharomyces cerevisiae type I phosphomannose isomerase assessed as D-mannose 6-phosphate to D-fructose 6-phosphate isomerization at pH 7.1 by PGI/G6PDH coupled enzyme spectrophotometric assay
- ChEBML_153319 In vitro inhibition of purine nucleoside phosphorylase from calf spleen in 1 mM phosphate
- ChEBML_65103 Competitive inhibitory activity with respect to EPSP (5-enolpyruvyl-shikimate- 3-phosphate) synthase
- ChEBML_72895 Inhibitory concentration against glyceraldehyde-3-phosphate dehydrogenase was determined as log 1/IC50
- ChEBML_90659 Inhibitory concentration against imidazole glycerol phosphate dehydratase (IGPD) from Cryptococcus neoformans
- ChEMBL_1455848 (CHEMBL887851) Inhibition of rat DNPH1 assessed as 2-deoxyribose 5-phosphate production by spectrophotometrically
- ChEMBL_1455849 (CHEMBL887852) Inhibition of human DNPH1 assessed as 2-deoxyribose 5-phosphate production by spectrophotometrically
- ChEMBL_1467560 (CHEMBL935628) Competitive inhibition of PTP1B (unknown origin) using p-nitrophenyl phosphate as substrate
- ChEMBL_147577 (CHEMBL657180) Accumulation of inositol phosphate in 1321N1 astrocytoma cells expressing human P2Y1 purinoceptor
- ChEMBL_1500296 (CHEMBL973438) Inverse agonist activity at rat ghrelin receptor by inositol phosphate turnover assay
- ChEMBL_1506090 (CHEMBL952471) Inhibition of human placental alkaline phosphatase using p-nitrophenyl phosphate substrate
- ChEMBL_153320 (CHEMBL876696) Inhibition of purine nucleoside phosphorylase from calf spleen in 50 mM phosphate
- ChEMBL_162032 (CHEMBL671798) Inhibition of calf spleen PNP (purine nucleoside phosphorylase) in 1 mM phosphate
- ChEMBL_162033 (CHEMBL671799) Inhibition of calf spleen PNP (purine nucleoside phosphorylase) in 50 mM phosphate
- ChEMBL_162190 (CHEMBL878136) Inhibition of human erythrocytic PNP (purine nucleoside phosphorylase) in 1 mM phosphate
- ChEMBL_1990679 (CHEMBL2443501) Inhibition of HSP90 ATPase activity (unknown origin) malachite-green phosphate assay
- ChEMBL_306074 (CHEMBL622813) Inhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cells
- ChEMBL_312533 (CHEMBL621965) Inhibition of PGD2-induced inositol phosphate formation at human Prostaglandin D2 receptor
- ChEMBL_399838 (CHEMBL706758) Inhibition of non-phosphorylated form of rabbit muscle glycogen phosphorylase in presence of phosphate
- ChEMBL_463125 (CHEMBL672271) Inhibition of human carbonic anhydrase 1 assessed as 4-nitrophenyl phosphate hydrolysis
- ChEMBL_463126 (CHEMBL672272) Inhibition of human carbonic anhydrase 2 assessed as 4-nitrophenyl phosphate hydrolysis
- ChEMBL_463127 (CHEMBL672273) Inhibition of mouse carbonic anhydrase 13 assessed as 4-nitrophenyl phosphate hydrolysis
- ChEMBL_504639 (CHEMBL620089) Inhibition of DNA polymerase beta lyase activity by deoxyribose phosphate excision assay
- ChEMBL_516599 (CHEMBL630107) Inhibition of fructose-1,6-bisphosphatase in mouse liver homogenates by colorimetric phosphate assay
- ChEMBL_566013 (CHEMBL674479) Inhibition of ATPase activity of SCV helicase assessed as phosphate release by colorimetric assay
- ChEMBL_598030 (CHEMBL706730) Inhibition of Streptococcus pneumoniae SP-3 gyrB by enzyme coupled phosphate assay
- ChEMBL_69909 (CHEMBL624925) Inhibitory concentration against Trypanosoma brucei glyceraldehyde-3-phosphate dehydrogenase (GAPDH)
- ChEMBL_69910 (CHEMBL624926) Inhibitory concentration against Trypanosoma brucei glyceraldehyde-3-phosphate dehydrogenase (GAPDH)
- ChEMBL_69911 (CHEMBL624927) Inhibitory concentration against Trypanosoma cruzi glyceraldehyde-3-phosphate dehydrogenase (GAPDH)
- ChEMBL_69912 (CHEMBL874402) Inhibitory concentration against Trypanosoma cruzi glyceraldehyde-3-phosphate dehydrogenase (GAPDH)
- ChEMBL_69913 (CHEMBL624928) Inhibitory concentration against Trypanosoma mexicana glyceraldehyde-3-phosphate dehydrogenase (GAPDH)
- ChEMBL_69915 (CHEMBL624930) Inhibitory concentration against rabbit muscle glyceraldehyde-3-phosphate dehydrogenase (GAPDH)
- ChEMBL_69916 (CHEMBL624931) Inhibitory concentration against rabbit muscle glyceraldehyde-3-phosphate dehydrogenase (GAPDH)
- ChEMBL_71454 (CHEMBL616577) Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
- ChEMBL_72770 (CHEMBL617766) Inhibitory activity measured for Glyceraldehyde-3-phosphate dehydrogenase (GAPDH) in Leishmania. mexicana
- ChEMBL_72772 (CHEMBL617768) Inhibitory activity was measured for Glyceraldehyde-3-phosphate dehydrogenase (GAPDH) in Leishmania. mexicana.
- ChEMBL_72905 (CHEMBL617621) Compound was tested for the inhibition of Leishmania mexicana GAPDH(glyceraldehyde-3-phosphate dehydrogenase)
- ChEMBL_741888 (CHEMBL655681) Inhibition of c-Kit after 45 mins by radiometric phosphate incorporation assay
- ChEMBL_831739 (CHEMBL644608) Inhibition of KHKC in human HepG2 cells assessed as level of fructose-1-phosphate
- ChEMBL_1499886 (CHEMBL976218) Antagonist activity at human glucocorticoid receptor transfected in CHOK1 cells assessed as inhibition of dexamethasone-induced receptor transcriptional activity after 6 hrs by luciferase reporter gene assay
- ChEMBL_634775 (CHEMBL644740) Antagonist activity at GR in human A549 cells transfected with luciferase gene linked to MMTV promoter assessed as inhibition of dexamethasone-induced luciferase transactivation activity after 24 hrs
- ChEMBL_728109 (CHEMBL875268) Agonist activity at GR expressed in african green monkey CV1 cells transfected with luciferase gene linked to MMTV promoter assessed as induction of luciferase transactivation activity relative to Dexamethasone
- ChEMBL_1670147 (CHEMBL1265357) Competitive inhibition of 6xHis-tagged human liver glycogen phosphorylase-a expressed in Escherichia coli BL21 Gold (DE3) assessed as release of inorganic phosphate using varying levels of glucose-1-phosphate and constant concentration of AMP and glycogen preincubated for 15 mins with AMP and glycogen followed by glucose-1-phosphate addition by Lineweaver-Burk plot method
- ChEMBL_1619019 (CHEMBL1101844) Inhibition of human recombinant liver glycogen phosphorylase A expressed in baculovirus infected Sf9 insect cells assessed as release of phosphate from glucose-1- phosphate in presence of 7.5 mM glucose by malachite green based assay
- ChEMBL_1630550 (CHEMBL1108264) Competitive inhibition of rabbit muscle glycogen phosphorylase-a assessed as release of inorganic phosphate using varying levels of glucose-1-phosphate and constant concentration of AMP and glycogen measured after 1 min by Dixon plot method
- ChEMBL_1924594 (CHEMBL3079258) Activation of human recombinant glucokinase using 5 mM glucose monitored over 5 mins in presence of NAD+ and glucose 6-phosphate 4% human serum albumin by glucose 6-phosphate dehydrogenase coupled assay
- ChEMBL_1759556 (CHEMBL1811082) Antagonist activity at glucocorticoid receptor (unknown origin) expressed in human ChaGoK1 cells assessed as inhibition of dexamethasone induced transactivation incubated for 24 hrs by beta-galactosidase reporter gene assay
- ChEMBL_1904911 (CHEMBL3064437) Antagonist activity at human glucocorticoid receptor expressed in CHO-K1 cells assessed as inhibition of glucocorticoid receptor-dexamethasone coactivator protein-protein interaction incubated for 24 hrs by bioluminescence assay
- Enzyme Inhibition Assay The activity of the compounds is determined by measuring the inhibitory effect of the compounds in the direction of glycogen synthesis, the conversion of glucose-1-phosphate into glycogen with the release of inorganic phosphate, which was monitored using microplate reader (BIO-RAD). The phosphate absorbance was measured at 655 nm. The IC50 values were estimated by fitting the inhibition data to a dose dependent curve using a logistic derivative equation.
- ChEBML_162111 Inhibitory potency for the protein tyrosine phosphatase (PTP 1B)-catalyzed hydrolysis of p-nitrophenol phosphate
- ChEBML_1685483 Inhibition of recombinant human PTP1B using p-nitrophenyl phosphate as substrate after 30 mins
- ChEBML_64958 Dissociation constant was calculated for Escherichia coli EPSP(5-enolpyruvyl-shikimate-3-phosphate) Synthase
- ChEBML_65094 The compound was tested for the inhibition of Escherichia coli 5-enolpyruvyl-shikimate-3-phosphate synthase (EPSP).
- ChEMBL_1367645 Inhibition of CDK1 (unknown origin) assessed as inhibition of phosphate incorporation into substrate in presence of radiolabeled ATP
- ChEMBL_1367646 Inhibition of CDK5 (unknown origin) assessed as inhibition of phosphate incorporation into substrate in presence of radiolabeled ATP
- ChEMBL_1367647 Inhibition of DYRK1A (unknown origin) assessed as inhibition of phosphate incorporation into substrate in presence of radiolabeled ATP
- ChEMBL_1367652 Inhibition of CLK1 (unknown origin) assessed as inhibition of phosphate incorporation into substrate in presence of radiolabeled ATP
- ChEMBL_1449753 (CHEMBL898858) Inhibition of rabbit skeletal muscle glycogen phosphorylase b assessed as inorganic phosphate release
- ChEMBL_1458320 (CHEMBL925651) Inhibition of SHP2 (unknown origin) using p-nitrophenyl phosphate substrate by microplate spectrophotometry
- ChEMBL_1462478 (CHEMBL928413) Inhibition of STEP (unknown origin) in absence of GSH by p-nitrophenyl phosphate hydrolysis assay
- ChEMBL_153319 (CHEMBL665702) In vitro inhibition of purine nucleoside phosphorylase from calf spleen in 1 mM phosphate
- ChEMBL_1548347 (CHEMBL1025013) Inhibition of human recombinant PTP1B using p-nitrophenyl phosphate as substrate by spectrophotometric analysis
- ChEMBL_1554435 (CHEMBL953924) Competitive inhibition of rabbit muscle glycogen phosphorylase b in presence of glucose 1-phosphate
- ChEMBL_1586214 (CHEMBL1053500) Inhibition of PTP1B (unknown origin) using p-nitrophenyl phosphate as substrate by colorimetric method
- ChEMBL_1586215 (CHEMBL1053501) Inhibition of TCPTP (unknown origin) using p-nitrophenyl phosphate as substrate by colorimetric method
- ChEMBL_1752096 (CHEMBL1786260) Agonist activity at P2Y2 receptor (unknown origin) assessed as reduction in inositol phosphate accumulation
- ChEMBL_1844001 Binding affinity to bovine beta-trypsin in phosphate/HEPES/Tricine/Tris buffer by ITC method
- ChEMBL_1844002 Binding affinity to human alpha-thrombin in phosphate/HEPES/Tricine/Tris buffer by ITC method
- ChEMBL_312848 (CHEMBL624027) Inhibition of U-46,619-induced inositol phosphate accumulation at human Thromboxane A2 receptor
- ChEMBL_322135 (CHEMBL639966) Effective concentration against US28-mediated inositol phosphate production in COS-7 cells
- ChEMBL_424478 (CHEMBL639244) Activity at human NK3 receptor assessed as stimulation of inositol phosphate generation in CHO cells
- ChEMBL_48586 (CHEMBL624211) Inhibition of inositol phosphate production induced by Cholecystokinin type B receptor (0.5 nM)
- ChEMBL_542431 (CHEMBL659181) Inhibition of human G6PDH using glucose-6-phosphate as substrate by Lineweaver-Burke plot
- ChEMBL_64950 (CHEMBL618971) Tested for the inhibition against Escherichia coli 5-enolpyruvyl-shikimate-3-phosphate synthase
- ChEMBL_72895 (CHEMBL617613) Inhibitory concentration against glyceraldehyde-3-phosphate dehydrogenase was determined as log 1/IC50
- ChEMBL_860252 (CHEMBL673038) Agonist activity at mouse GPR142 expressed in HEK293 cells by inositol phosphate accumulation assay
- ChEMBL_90659 (CHEMBL616007) Inhibitory concentration against imidazole glycerol phosphate dehydratase (IGPD) from Cryptococcus neoformans
- ChEMBL_90660 (CHEMBL616008) Binding affinity imidazole glycerol phosphate dehydratase (IGPD) obtained from Cryptococcus neoformans
- Enzyme Assay The rate of carbamoyl phosphate synthesis was determined by use of a coupled enzyme assay with ornithine transcarbamoylase.
- ChEMBL_767067 (CHEMBL674699) Inhibition of Mycobacterium tuberculosis DXR assessed as reduction of 1-deoxy-D-xylulose 5-phosphate into 2-C-methyl-D-erythritol-4-phosphate measured for every 5 secs upto 500 secs by spectrophotometry analysis
- ChEMBL_631316 (CHEMBL644869) Inhibition of dexamethasone-induced human NR1-1a/NR2A receptor-mediated excitotoxicity in (S)-glutamate/glycine-stimulated mouse L12-G10 cells assessed as LDH release after 30 mins
- ChEMBL_631318 (CHEMBL644871) Inhibition of dexamethasone-induced human NR1-1a/NR2B receptor-mediated excitotoxicity in (S)-glutamate/glycine-stimulated mouse L13-E6 cells assessed as LDH release after 30 mins
- ChEBML_153324 Inhibition of Purine nucleoside phosphorylase was evaluated against the enzyme from calf spleen in 50 mM phosphate
- ChEBML_153325 Inhibition of Purine nucleoside phosphorylase was evaluated against the enzyme from Human erythrocytic in 50 mM phosphate
- ChEBML_1651766 Inhibition of recombinant human ATX using bisP-nitrophenyl phosphate as substrate measured after 30 mins
- ChEBML_1717872 Inhibition of PTP1B (unknown origin) using p-nitrophenyl phosphate as substrate measured after 30 mins
- ChEBML_64947 Compound was tested for inhibitory activity against EPSP(5-enolpyruvylshikimate 3-phosphate) synthase in Escherichia coli.
- ChEBML_65093 Tested for the inhibition against Escherichia coli 5-enolpyruvyl-shikimate-3-phosphate synthase versus phosphoenolpyruvate
- ChEBML_70678 KI for pyridoxal 5'-phosphate (PLP)-dependent Gamma-amino-N-butyrate transaminase at pH 7.4
- ChEMBL_1288272 Inhibition of mouse EAP using p-nitrophenyl phosphate as substrate after 30 mins by chemiluminescence assay
- ChEMBL_1335408 (CHEMBL862016) Inhibition of PTP1B (unknown origin) using nitrophenyl phosphate as substrate after 30 mins by spectrophotometry
- ChEMBL_1362995 (CHEMBL871258) Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
- ChEMBL_1449543 (CHEMBL899809) Inhibition of rabbit muscle glycogen phosphorylase b at pH 6.8 assessed as inorganic phosphate release
- ChEMBL_1461022 (CHEMBL944978) Inhibition of PRL3 (unknown origin) using DiFMUP as fluorogenic phosphate substrate assessed as DiFMUP dephosphorylation
- ChEMBL_1461023 (CHEMBL944055) Inhibition of PRL2 (unknown origin) using DiFMUP as fluorogenic phosphate substrate assessed as DiFMUP dephosphorylation
- ChEMBL_1461024 (CHEMBL944056) Inhibition of PRL1 (unknown origin) using DiFMUP as fluorogenic phosphate substrate assessed as DiFMUP dephosphorylation
- ChEMBL_1476393 (CHEMBL929386) Inhibition of recombinant human PTP1B using p-nitrophenyl phosphate as substrate after 40 mins
- ChEMBL_1497576 (CHEMBL999423) Inhibition of PTP1B (unknown origin) using p-nitrophenyl phosphate as substrate after 30 mins
- ChEMBL_153321 (CHEMBL665703) Inhibition of purine nucleoside phosphorylase against the enzyme from calf spleen in 1 mM phosphate
- ChEMBL_1575591 (CHEMBL1036436) Inhibition of human sphingosine 1-phosphate lyase after 22 hrs by umbelliferone fluorescence analysis
- ChEMBL_1586209 (CHEMBL1053495) Inhibition of human TCPTP using p-nitrophenyl phosphate as substrate by micro plate reader method
- ChEMBL_1705037 (CHEMBL1661472) Inhibition of PTP1B (unknown origin) using p-nitrophenyl phosphate substrate incubated for 30 mins
- ChEMBL_1705038 (CHEMBL1661473) Inhibition of SHP2 (unknown origin) using p-nitrophenyl phosphate substrate incubated for 30 mins
- ChEMBL_1705039 (CHEMBL1661474) Inhibition of PTPLAR (unknown origin) using p-nitrophenyl phosphate substrate incubated for 30 mins
- ChEMBL_1705040 (CHEMBL1661475) Inhibition of TCPTP (unknown origin) using p-nitrophenyl phosphate substrate incubated for 30 mins
- ChEMBL_1746765 (CHEMBL1776934) Inhibition of SHP2 (unknown origin) using 3-o-methylfluorescein phosphate as substrate by fluorescence assay
- ChEMBL_1746770 (CHEMBL1776939) Inhibition of SHP1 (unknown origin) using 3-o-methylfluorescein phosphate as substrate by fluorescence assay
- ChEMBL_1986994 (CHEMBL2439314) Inhibition of SHP2 (unknown origin) using 3-o-methylfluorescein phosphate as substrate by fluorescence assay
- ChEMBL_1986997 (CHEMBL2439317) Inhibition of SHP1 (unknown origin) using 3-o-methylfluorescein phosphate as substrate by fluorescence assay
- ChEMBL_2015157 (CHEMBL632818) Inhibition of human CD73 using AMP as substrate by Malachite green phosphate reagent-based assay
- ChEMBL_208010 (CHEMBL621401) Inhibition of HSV-1 thymidine kinase, 1 uM [3H]thymidine and ATP as phosphate donor
- ChEMBL_208029 (CHEMBL618452) Inhibition of HSV-2 thymidine kinase, 2 uM [3H]thymidine and ATP as phosphate donor
- ChEMBL_303534 (CHEMBL619201) In vitro inhibitory concentration against Protein-tyrosine phosphatase 1B hydrolysis of p-nitrophenol phosphate
- ChEMBL_306715 (CHEMBL619490) Inhibitory concentration against human glutathione reductase in the absence of glucose-6-phosphate dehydrogenase (G6PDH)
- ChEMBL_306877 (CHEMBL623328) Inhibition of CCK-Induced inositol phosphate production in Cos-7 cells expressing human CCK1R
- ChEMBL_317580 (CHEMBL630505) Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I352A)
- ChEMBL_317584 (CHEMBL630509) Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (F107A)
- ChEMBL_317585 (CHEMBL875289) Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329A)
- ChEMBL_317586 (CHEMBL630510) Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329F)
- ChEMBL_317587 (CHEMBL630511) Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I352A)
- ChEMBL_317588 (CHEMBL631404) Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (M195L)
- ChEMBL_317589 (CHEMBL631405) Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R197M)
- ChEMBL_317590 (CHEMBL631406) Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R336M)
- ChEMBL_317591 (CHEMBL631407) Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S342A)
- ChEMBL_317592 (CHEMBL631408) Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S348A)
- ChEMBL_317593 (CHEMBL631409) Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (T117A)
- ChEMBL_382561 (CHEMBL691701) Inhibition of kinesin ATPase activity by enzyme-linked inorganic phosphate detection assay without preincubation
- ChEMBL_424431 (CHEMBL642791) Activity at human NK3 receptor expressed in CHO cells assessed as increase in inositol phosphate generation
- ChEMBL_430293 (CHEMBL639463) Displacement of [33P]sphingosine 1 phosphate from human S1P1 receptor expressed in CHO cells
- ChEMBL_430294 (CHEMBL639464) Displacement of [33P]sphingosine 1 phosphate from human S1P2 receptor expressed in CHO cells
- ChEMBL_430295 (CHEMBL875505) Displacement of [33P]sphingosine 1 phosphate from human S1P3 receptor expressed in CHO cells
- ChEMBL_430296 (CHEMBL639465) Displacement of [33P]sphingosine 1 phosphate from human S1P4 receptor expressed in CHO cells
- ChEMBL_430297 (CHEMBL639466) Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells
- ChEMBL_542429 (CHEMBL659179) Inhibition of Trypanosoma brucei G6PDH using glucose-6-phosphate as substrate by Lineweaver-Burke plot
- ChEMBL_581483 (CHEMBL687856) Inhibition of ATPase activity of SARS coronavirus helicase assessed as phosphate release by malachite green assay
- ChEMBL_590794 (CHEMBL701641) Agonist activity at human NK3 receptor expressed in cells assessed as accumulation of [3H]inositol phosphate
- ChEMBL_598343 (CHEMBL706505) Inhibition of recombinant human PTP1B assessed as hydrolysis of p-nitrophenyl phosphate after 30 mins
- ChEMBL_602838 (CHEMBL621524) Antagonist activity at human mGluR5 assessed as inhibition of quisqualate-induced intracellular inositol phosphate accumulation
- ChEMBL_63499 (CHEMBL619169) Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin A receptor of MMQ cells.
- ChEMBL_64958 (CHEMBL618978) Dissociation constant was calculated for Escherichia coli EPSP(5-enolpyruvyl-shikimate-3-phosphate) Synthase
- ChEMBL_64961 (CHEMBL618981) Tested for the dissociation constant against Escherichia coli 5-enolpyruvyl-shikimate-3-phosphate synthase
- ChEMBL_64963 (CHEMBL620150) The compound was tested for the inhibition of Escherichia coli 5-enolpyruvyl-shikimate-3-phosphate synthase (EPSP).
- ChEMBL_65087 (CHEMBL624374) Binding affinity against Escherichia coli EPSP(5-enolpyruvyl-shikimate-3-phosphate) synthase
- ChEMBL_65094 (CHEMBL624562) The compound was tested for the inhibition of Escherichia coli 5-enolpyruvyl-shikimate-3-phosphate synthase (EPSP).
- ChEMBL_65099 (CHEMBL624566) Tested for the dissociation rate against Escherichia coli 5-enolpyruvyl-shikimate-3-phosphate synthase
- ChEMBL_65101 (CHEMBL624567) Tested for the rate of association against Escherichia coli 5-enolpyruvyl-shikimate-3-phosphate synthase
- ChEMBL_70746 (CHEMBL615851) Inhibition of rat brain farnesyltransferase in 5 mM potassium phosphate and 50 mM HEPES buffer
- ChEMBL_72880 (CHEMBL617783) Tested for the inhibitory activity against Glycosomal glyceraldehyde 3-phosphate dehydrogenase (gGAPDH) of Leishmania mexicana
- ChEMBL_72889 (CHEMBL617791) Tested for the inhibitory activity against Glycosomal glyceraldehyd 3-phosphate dehydrogenase (gGAPDH) of Trypanosoma brucei
- ChEMBL_72890 (CHEMBL617608) Tested for the inhibitory activity against Glycosomal glyceraldehyde 3-phosphate dehydrogenase (gGAPDH) of Trypanosoma brucei
- ChEMBL_72902 (CHEMBL617618) Tested for the inhibitory activity against Glycosomal glyceraldehyde 3-phosphate dehydrogenase (gGAPDH) of human erythrocyte
- ChEMBL_743338 (CHEMBL650613) Inhibition of full length recombinant ATR after 24 hrs by radiometric phosphate incorporation assay
- ChEMBL_743383 (CHEMBL653187) Inhibition of full length recombinant ATM after 24 hrs by radiometric phosphate incorporation assay
- ChEMBL_744737 (CHEMBL656095) Agonist activity at human 5HT2C receptor expressed in HEK293 cells by inositol phosphate accumulation assay
- ChEMBL_744739 (CHEMBL656097) Agonist activity at human 5HT2B receptor expressed in HEK293 cells by inositol phosphate accumulation assay
- ChEMBL_748961 (CHEMBL661673) Inhibition of recombinant human PTP1B using p-nitrophenyl phosphate as substrate after 30 mins
- ChEMBL_753876 (CHEMBL660719) Inhibition of Calmodulin-dependent PDE1 activity assessed as inorganic phosphate release after 30 min
- ChEMBL_802298 (CHEMBL617083) Inhibition of rabbit muscle glycogen phosphorylase b assessed as inorganic phosphate release at pH 6.8
- ChEMBL_839558 (CHEMBL654216) Agonist activity at P2Y6 receptor expressed in human 1321N1 cells assessed as inositol phosphate accumulation
- ChEMBL_856703 (CHEMBL672076) Inhibition of human recombinant PTP1B using p-nitrophenyl phosphate as substrate after 30 mins
- ChEMBL_862643 (CHEMBL676688) Inhibition of human glucose-6-phosphate dehydrogenase after 90 mins by resazurin/diaphorasecoupled assay
- ChEMBL_862644 (CHEMBL676689) Inhibition of Plasmodium falciparum glucose-6-phosphate dehydrogenase after 45 mins by orthogonal assay
- ChEMBL_728111 (CHEMBL644024) Agonist activity at GR expressed in IL-1beta- and TNFalpha-stimulated HepG2 cells assessed as inhibition of NFKB- or AP-1 mediated E-selectin transcription by luciferase reporter gene assay relative to Dexamethasone
- ChEMBL_1670149 (CHEMBL1265359) Competitive inhibition of rabbit muscle glycogen phosphorylase-a in presence of varying levels of glucose-1-phosphate and constant concentration of glycogen and AMP preincubated for 15 mins with AMP and glycogen followed by glucose-1-phosphate addition by Lineweaver-Burk plot method
- ChEMBL_1670148 (CHEMBL1265358) Competitive inhibition of rabbit muscle glycogen phosphorylase-b in presence of varying levels of glucose-1-phosphate and constant concentration of glycogen and AMP preincubated for 15 mins with AMP and glycogen followed by glucose-1-phosphate addition by Lineweaver-Burk plot method
- GR Binding Assay and GRAF Assay For compounds able to displace the 3(H)-dexamethasone from the receptor an IC50 value (the concentration required to inhibit 50% of the binding of 3(H)-dex) was determined by a nonlinear four parameter logistic model. The EC50s are the concentrations of compounds required to inhibit 50% of dexamethasone-induced alkaline phosphatase (ALP) expression in GRAF cell line, which is produced by CHO-K1 cells stably transfected with GR and a reporter construct containing a glucocorticoid response element driving expression of ALP.
- GR Binding Assay and Human IL-6 Assay The IC50s were determined by incubating the receptors with radiolabeled dexamethasone in the presence of full log scale concentrations (10-11 M to 10-6 M) of cold dexamethasone or the ligands. The IC50s were calculated assuming a single binding site sigmoidal dose-response model. The EC50s were obtained from transcriptional repression of IL-6-release using the human A549 lung epithelial cell line and freshly isolated mouse thioglycolate-elicited peritoneal exudate cells.
- ChEMBL_1361029 Antagonist activity at human recombinant 5-HT2A receptor assessed as inhibition of serotonin-induced inositol phosphate accumulation
- ChEMBL_1361031 Antagonist activity at human recombinant 5-HT2C receptor assessed as inhibition of serotonin-induced inositol phosphate accumulation
- ChEMBL_1363386 Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay
- ChEMBL_1500295 (CHEMBL970507) Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by inositol phosphate turnover assay
- ChEMBL_1520498 (CHEMBL948844) Binding affinity to Grb7-SH2 domain (unknown origin) without using phosphate buffer by SPR analysis
- ChEMBL_153322 (CHEMBL664908) Inhibition of Purine nucleoside phosphorylase was evaluated against the enzyme from calf spleen in 50 mM phosphate
- ChEMBL_153323 (CHEMBL664909) Inhibition of Purine nucleoside phosphorylase was evaluated against the enzyme from calf spleen in 1 mM phosphate
- ChEMBL_153324 (CHEMBL664910) Inhibition of Purine nucleoside phosphorylase was evaluated against the enzyme from calf spleen in 50 mM phosphate
- ChEMBL_1538843 (CHEMBL1033086) Inhibition of GPAT1 (unknown origin) by CPM assay using glycerol-3-phosphate and oleoyl-CoA as substrate
- ChEMBL_1546979 (CHEMBL1032591) Binding affinity to Salmonella typhi glucose-1-phosphate cytidylyl-transferase assessed as dissociation constant by spectrophotometry
- ChEMBL_1619017 (CHEMBL1101842) Inhibition of rabbit muscle glycogen phosphorylase b using alpha-D-glucose-1-phosphate as substrate
- ChEMBL_1651766 (CHEMBL1225382) Inhibition of recombinant human ATX using bisP-nitrophenyl phosphate as substrate measured after 30 mins
- ChEMBL_1767106 (CHEMBL1826155) Inhibition of recombinant human GST-tagged PTP1B catalytic domain using para-nitrophenyl phosphate as substrate
- ChEMBL_2168507 (CHEMBL773821) Inhibition of human SHIP2 (419 to 732 residues) expressed in Escherichia coli by malachite green phosphate assay
- ChEMBL_216946 (CHEMBL629381) Inhibitory potency for brewer's yeast alpha-glucosidase in 0.1 M sodium phosphate buffer at pH 6.55.
- ChEMBL_29964 (CHEMBL877491) 50% inhibition of human placental alkaline phosphatase in the presence of 10 mM p-nitrophenyl phosphate as substrate
- ChEMBL_361236 (CHEMBL674355) Antagonist activity at human recombinant GnRH receptor assessed as inhibition of GnRH-stimulated inositol phosphate accumulation
- ChEMBL_361237 (CHEMBL674356) Antagonist activity at rat pituitary GnRH receptor assessed as inhibition of GnRH-stimulated inositol phosphate accumulation
- ChEMBL_399839 (CHEMBL874155) Inhibition of non-phosphorylated form of rabbit muscle glycogen phosphorylase in presence of glycogen and 45 mM phosphate
- ChEMBL_399840 (CHEMBL706759) Inhibition of non-phosphorylated form of rabbit muscle glycogen phosphorylase in presence of 6.17 mM glycogen and phosphate
- ChEMBL_424432 (CHEMBL642792) Antagonist activity at human NK3 receptor expressed in CHO cells assessed as inhibition of inositol phosphate generation
- ChEMBL_424463 (CHEMBL638531) Activity at human NK3 receptor assessed as inhibition of senktide-stimulated inositol phosphate generation in CHO cells
- ChEMBL_440404 (CHEMBL651645) Agonist activity at mGlu4 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate production
- ChEMBL_440405 (CHEMBL651646) Agonist activity at mGlu6 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate production
- ChEMBL_440406 (CHEMBL651647) Agonist activity at mGlu7 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate production
- ChEMBL_440407 (CHEMBL651850) Agonist activity at mGlu8 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate production
- ChEMBL_445954 (CHEMBL662664) Agonist activity at rat mGluR4 receptor expressed HEK293 cells assessed as effect on inositol phosphate production
- ChEMBL_445955 (CHEMBL874521) Agonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate production
- ChEMBL_445956 (CHEMBL858316) Agonist activity at rat mGluR7 receptor expressed HEK293 cells assessed as effect on inositol phosphate production
- ChEMBL_445957 (CHEMBL662665) Agonist activity at rat mGluR8 receptor expressed HEK293 cells assessed as effect on inositol phosphate production
- ChEMBL_457690 (CHEMBL669968) Antagonist activity at human CRTH2 receptor assessed as inhibition of PGD2-induced signaling by inositol-phosphate assay
- ChEMBL_460661 (CHEMBL671698) Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
- ChEMBL_590795 (CHEMBL701642) Agonist activity at guinea pig NK3 receptor expressed in cells assessed as accumulation of [3H]inositol phosphate
- ChEMBL_64947 (CHEMBL618968) Compound was tested for inhibitory activity against EPSP(5-enolpyruvylshikimate 3-phosphate) synthase in Escherichia coli.
- ChEMBL_64955 (CHEMBL618976) Compound was tested for inhibitory activity against EPSP(5-enolpyruvylshikimate 3-phosphate) synthase in Escherichia coli.
- ChEMBL_64960 (CHEMBL618980) Inhibitory activity was evaluated against Escherichia coli EPSP(5-enolpyruvyl-shikimate-3-phosphate) Synthase
- ChEMBL_65086 (CHEMBL624373) Compound was tested for inhibitory activity against EPSP(5-enolpyruvylshikimate 3-phosphate) synthase in Escherichia coli.
- ChEMBL_65093 (CHEMBL624561) Tested for the inhibition against Escherichia coli 5-enolpyruvyl-shikimate-3-phosphate synthase versus phosphoenolpyruvate
- ChEMBL_65096 (CHEMBL624564) Compound was tested for inhibitory activity against EPSP(5-enolpyruvylshikimate 3-phosphate) synthase in Escherichia coli.
- ChEMBL_754327 (CHEMBL669390) Inhibition of human recombinant PTP1B assessed as inhibition of para-nitrophenyl phosphate to para-nitrophenol conversion by spectrophotometry
- ChEMBL_798051 (CHEMBL704463) Inhibition of PTP1B assessed as para-nitrophenyl phosphate catalyzed hydrolysis of para-nitrophenol by p-NPP assay
- ChEMBL_801146 (CHEMBL616091) Inhibition of Mycobacterium tuberculosis PTP-A using p-nitrophenyl phosphate as substrate measured for 10 mins by spectrofluorimetry
- ChEMBL_831490 (CHEMBL649799) Inhibition of GST-tagged human recombinant PTP1B using para-nitrophenyl phosphate as substrate by spectrophotometric analysis
- ChEMBL_862647 (CHEMBL872894) Inhibition of Plasmodium falciparum glucose-6-phosphate dehydrogenase after 2 hrs by resazurin/diaphorasecoupled assay
- Competitive Inhibition Assay PNPase activity (guanosine to guanine and ribose 1-phosphate) was followed by measuring the decrease in absorbance at 268nm.
- ChEMBL_1630554 (CHEMBL1108268) Competitive inhibition of rabbit muscle glycogen phosphorylase-b assessed as release of inorganic phosphate using varying levels of glucose-1-phosphate and constant concentration of AMP and glycogen measured at 1 min time interval for 1 to 5 mins by Hill plot method
- ChEMBL_2027541 (CHEMBL636119) Inhibition of active recombinant human N-terminal His-tagged 11-betaHSD1 expressed in Escherichia coli using cortisone, NADPH and glucose-6-phosphate incubated for 2 hrs by glucose-6-phosphate dehydrogenase based coupled HTRF immuno-competitive assay
- ChEMBL_1497288 (CHEMBL995850) Antagonist activity at human glucocorticoid receptor expressed in CHOK1 cells assessed as inhibition of dexamethasone-induced protein interaction with steroid receptor co-activator peptide after overnight incubation by beta-galactosidase reporter gene assay
- Inhibition Assay Pooled human liver microsome suspension (20 mg/mL) was diluted with phosphate buffer to obtain a 5 mg/mL suspension. A solution of NADPH was prepared in phosphate buffer at a concentration of 5 mM. Separate stock solutions of each substrate were prepared in DMSO:MeCN (50:50 v/v), mixed, and diluted in phosphate buffer to obtain a single solution containing each substrate at five times its experimentally determined Km concentration.
- ChEBML_143203 Agonistic activity was determined against human Neuromedin B receptor transfected in HEK293 cells as accumulation levels of inositol phosphate
- ChEBML_219283 Ability to inhibit yeast glyoxalase I enzyme in 0.05 M phosphate buffer, pH 6.6, 30 degree C
- ChEBML_32781 Dissociation constant in high affinity sites where the binding is in 50 mM phosphate buffer for Alpha-2 adrenergic receptor
- ChEBML_32783 Dissociation constant in low affinity sites where the binding is in 50 mM phosphate buffer for Alpha-2 adrenergic receptor
- ChEMBL_1288117 Competitive inhibition Trypanosoma brucei PFK using fructose-6-phosphate as substrate by Line-weaver Burk plot analysis
- ChEMBL_1436200 (CHEMBL905605) Inhibition of Mycobacterium tuberculosis IspC using 1-deoxy-D-xylulose 5-phosphate as substrate by photometric analysis
- ChEMBL_1448918 (CHEMBL898046) Inhibition of PHOSPHO1 phosphoethanolamine activity (unknown origin) assessed as amount of inorganic phosphate release after 30 mins
- ChEMBL_145032 (CHEMBL658030) Ability to inhibit OT-induced inositol phosphate accumulation was determined in CHO cells expressing the human OT receptor
- ChEMBL_1476391 (CHEMBL929384) Inhibition of recombinant human PTP1B (1 to 299) expressed in Escherichia coli using p-nitrophenyl phosphate as substrate
- ChEMBL_1476723 (CHEMBL933513) Agonist activity at rat mGluR2 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
- ChEMBL_1476724 (CHEMBL921414) Agonist activity at rat mGluR4 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
- ChEMBL_1476726 (CHEMBL921416) Agonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
- ChEMBL_1476727 (CHEMBL921417) Agonist activity at rat mGluR7 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
- ChEMBL_1476728 (CHEMBL921418) Agonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
- ChEMBL_1476729 (CHEMBL921419) Agonist activity at rat mGluR1 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
- ChEMBL_1476730 (CHEMBL921420) Agonist activity at rat mGluR5 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
- ChEMBL_1520499 (CHEMBL948845) Binding affinity to Grb7-SH2 domain (unknown origin) using 100 mM phosphate buffer by SPR analysis
- ChEMBL_1566144 (CHEMBL960061) Inhibition of recombinant human PTP-1B expressed in Escherichia coli TB1 using p-nitrophenyl phosphate as substrate
- ChEMBL_1586211 (CHEMBL1053497) Inhibition of human recombinant PTP1B expressed in Escherichia coli using p-nitrophenyl phosphate as substrate by UV spectroscopy
- ChEMBL_162594 (CHEMBL673122) Inhibitory effect against protein-tyrosine phosphatase Lar, using p-nitrophenyl phosphate as substrate at pH 5.5.
- ChEMBL_1630545 (CHEMBL1108259) Competitive inhibition of rabbit muscle glycogen phosphorylase-b in presence of varying glucose-1-phosphate levels and NADP
- ChEMBL_1793242 (CHEMBL1931637) Competitive inhibition of Mycobacterium tuberculosis PtpA using p-nitrophenyl phosphate as substrate by Michaelis-Menten plot analysis
- ChEMBL_201317 (CHEMBL616694) Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 1 expressed on CHO cell membranes
- ChEMBL_201334 (CHEMBL616960) Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 3 expressed on CHO cell membranes
- ChEMBL_201335 (CHEMBL616961) Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 4 expressed on CHO cell membranes
- ChEMBL_201454 (CHEMBL616577) Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
- ChEMBL_2130000 (CHEMBL741427) Inhibition of SLK (unknown origin) assessed as transfer of radiolabelled phosphate group from ATP by reaction biology method
- ChEMBL_2130002 (CHEMBL741429) Inhibition of CLK2 (unknown origin) assessed as transfer of radiolabelled phosphate group from ATP by reaction biology method
- ChEMBL_2130003 (CHEMBL741430) Inhibition of GSK3alpha (unknown origin) assessed as transfer of radiolabelled phosphate group from ATP by reaction biology method
- ChEMBL_2130004 (CHEMBL741431) Inhibition of GSK3beta (unknown origin) assessed as transfer of radiolabelled phosphate group from ATP by reaction biology method
- ChEMBL_304296 (CHEMBL618405) Effective concentration against sphingosine-1-phosphate receptor 1 determined by a [c-35S]-GTP binding assay
- ChEMBL_304306 (CHEMBL618415) Effective concentration against sphingosine 1-phosphate receptor 2 determined by a [c-35S]-GTP binding assay
- ChEMBL_304307 (CHEMBL618416) Effective concentration against sphingosine 1-phosphate receptor 3 determined by a [c-35S]-GTP binding assay
- ChEMBL_304308 (CHEMBL876401) Effective concentration against sphingosine 1-phosphate receptor 4 determined by a [c-35S]-GTP binding assay
- ChEMBL_304309 (CHEMBL618417) Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay
- ChEMBL_304324 (CHEMBL883799) Effective concentration to activate wild-type P2Y1 receptor expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_306053 (CHEMBL625246) Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 1 expressed on CHO cell membranes
- ChEMBL_306054 (CHEMBL625247) Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 2 expressed on CHO cell membranes
- ChEMBL_306055 (CHEMBL625248) Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 3 expressed on CHO cell membranes
- ChEMBL_306056 (CHEMBL625249) Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 4 expressed on CHO cell membranes
- ChEMBL_306057 (CHEMBL625250) Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes
- ChEMBL_313020 (CHEMBL631436) Inhibition of PGD2-induced inositol phosphate formation at human chemoattractant receptor-homologous molecule expressed on TH2 cells
- ChEMBL_382280 (CHEMBL690823) Activity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulation
- ChEMBL_382560 (CHEMBL691700) Inhibition of kinesin ATPase activity by enzyme-linked inorganic phosphate detection assay with 5 mins pre-incubation
- ChEMBL_40068 (CHEMBL615190) Inhibitory effect against human CD45 tyrosine phosphatase using p-nitrophenyl phosphate substrate at a pH 7.0
- ChEMBL_447478 (CHEMBL660170) Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
- ChEMBL_481449 (CHEMBL691956) Inhibition of lyase activity of rat DNA polymerase beta after 30 mins by deoxyribose phosphate excision assay
- ChEMBL_535725 (CHEMBL652795) Inhibition of Mycobacterium tuberculosis cloned 1-deoxy-D-xylulose-5-phosphate synthase expressed in Escherichia coli
- ChEMBL_543916 (CHEMBL659475) Inhibition of recombinant calmodulin mediated bovine brain PDE1 activation assessed as effect on inorganic phosphate release by spectrophotometry
- ChEMBL_556099 (CHEMBL665405) Agonist activity at rat 5HT2A receptor expressed in mouse NIH3T3 cells assessed as stimulation of inositol phosphate accumulation
- ChEMBL_559825 (CHEMBL675137) Binding affinity to PSMA in human LNCaP cells assessed as cell surface binding in phosphate-buffered saline buffer
- ChEMBL_559827 (CHEMBL675139) Binding affinity to PSMA in human PC3 cells assessed as cell surface binding in phosphate-buffered saline buffer
- ChEMBL_600348 (CHEMBL615321) Agonist activity at 5HT2A receptor expressed in HEK cells assessed as inhibition of serotonin-induced inositol phosphate accumulation
- ChEMBL_610374 (CHEMBL627820) Inhibition of SHP1 expressed in Escherichia coli assessed as inhibition of p-nitrophenyl phosphate hydrolysis at pH 7 by spectrophotometry
- ChEMBL_610375 (CHEMBL627821) Inhibition of PTP1B expressed in Escherichia coli assessed as inhibition of p-nitrophenyl phosphate hydrolysis at pH 7 by spectrophotometry
- ChEMBL_610376 (CHEMBL628464) Inhibition of HePTP expressed in Escherichia coli assessed as inhibition of p-nitrophenyl phosphate hydrolysis at pH 7 by spectrophotometry
- ChEMBL_610377 (CHEMBL626239) Inhibition of Lyp expressed in Escherichia coli assessed as inhibition of p-nitrophenyl phosphate hydrolysis at pH 7 by spectrophotometry
- ChEMBL_610378 (CHEMBL626240) Inhibition of FAP1 expressed in Escherichia coli assessed as inhibition of p-nitrophenyl phosphate hydrolysis at pH 7 by spectrophotometry
- ChEMBL_610379 (CHEMBL626241) Inhibition of CD45 expressed in Escherichia coli assessed as inhibition of p-nitrophenyl phosphate hydrolysis at pH 7 by spectrophotometry
- ChEMBL_610380 (CHEMBL626242) Inhibition of LAR expressed in Escherichia coli assessed as inhibition of p-nitrophenyl phosphate hydrolysis at pH 7 by spectrophotometry
- ChEMBL_610381 (CHEMBL626243) Inhibition of PTPalpha expressed in Escherichia coli assessed as inhibition of p-nitrophenyl phosphate hydrolysis at pH 7 by spectrophotometry
- ChEMBL_610382 (CHEMBL626244) Inhibition of VHR expressed in Escherichia coli assessed as inhibition of p-nitrophenyl phosphate hydrolysis at pH 7 by spectrophotometry
- ChEMBL_610383 (CHEMBL626907) Inhibition of Cdc14A expressed in Escherichia coli assessed as inhibition of p-nitrophenyl phosphate hydrolysis at pH 7 by spectrophotometry
- ChEMBL_610384 (CHEMBL626908) Inhibition of LMWPTP expressed in Escherichia coli assessed as inhibition of p-nitrophenyl phosphate hydrolysis at pH 7 by spectrophotometry
- ChEMBL_612567 (CHEMBL628485) Activity at human 5HT2A receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation counting
- ChEMBL_634153 (CHEMBL649898) Inverse agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of inositol phosphate accumulation
- ChEMBL_662795 (CHEMBL674108) Antagonist activity at human bradykinin B1 receptor in human MR5 cells assessed as [3H]inositol phosphate accumulation
- ChEMBL_801147 (CHEMBL616092) Inhibition of Mycobacterium tuberculosis PTP-B using p-nitrophenyl phosphate as substrate measured for 10 mins by spectrofluorimetry
- ChEMBL_821949 (CHEMBL636467) Inhibition of human Tdp1 using 3'-phosphate-(4-methylumbelliferone)-thymidine as substrate after 180 mins by spectrophotometry
- ChEMBL_886806 (CHEMBL694031) Inhibition of human recombinant PTP1B using p-nitrophenyl phosphate as substrate after 30 mins by spectrophotometric analysis
- ChEMBL_962306 (CHEMBL675228) Inhibition of human recombinant GST-tagged PTP1B using para-nitrophenyl phosphate as substrate after 2 mins
- ChEMBL_972706 (CHEMBL683943) Agonist activity at human GPR142 transfected in HEK293 cells after 1 hr by inositol phosphate accumulation assay
- NMR (OBClip) The experimental studies were carried out in 20 mM sodium phosphate buffer at pH7.4, at a temperature of 298 K.
- PKA assay The activity of PKA, activated by cAMP, is measured by its ability to transfer phosphate from [gamma-32P]ATP to histone.
- UV/VIS The experimental studies were carried out in 20 mM sodium phosphate buffer at pH7.4, at a temperature of 298 K.
- cGPK assay The activity of cGPK, activated by cGMP, is measured by its ability to transfer phosphate from [gamma-32P]ATP to histone.
- Receptor Binding Assay Binding Assay (I):In order to assess the affinity of test compounds for the human glucocorticoid receptor, a commercially available kit was used (Glucocorticoid Receptor Competitor Assay Kit, Invitrogen Part #2893). Briefly, purified human recombinant full-length glucocorticoid receptor (2 nM) was mixed with fluorescently labeled glucocorticoid (1 nM Fluormone GS Red) in the presence or absence of test compound. After two hour incubation at room temperature in the dark, the fluorescence polarization (FP) of the samples was measured. The FP of a mixture of receptor, fluorescent probe (i.e., Fluormone GS Red) and 5 μM dexamethasone represented background fluorescence or 100% inhibition, whereas, the FP of the mixture without dexamethasone (but in the presence of vehicle) was taken to be 100% binding. The percentage inhibition of test compounds were then compared to the sample with 5 μM dexamethasone and expressed as % relative binding activity with dexamethasone being 100% and no inhibition is 0%. Test compounds were analyzed in the concentration range from 8.5E-05 μM to 5 μM. Binding Assay (II):In order to measure the binding of compounds on the glucocorticoid receptor a commercially available kit was used (Glucocorticoid receptor competitor assay kit, PanVera Co., Madison, Wis., P2816). Briefly, a cell lysate containing recombinantly expressed human full-length glucocorticoid receptor was mixed with a fluorescently labeled glucocorticoid (1 nM Fluormone GS1) in the presence or absence of test compound. After one hour at room temperature, the fluorescence polarization (FP) of the samples were measured. The FP of a mixture of receptor, fluorescent probe (i.e., Fluormone GS1) and 1 mM dexamethasone represented background fluorescence or 100% inhibition, whereas, the FP of the mixture without dexamethasone was taken to be 100% binding. The percentage inhibition of test molecules were then compared to the sample with 1 mM dexamethasone and expressed as % relative binding activity with dexamethasone being 100% and no inhibition is 0%. Test molecules were analyzed in the concentration range from 2.4 nM to 40 μM.Site I binding assays for any NHR (Nuclear Hormone Receptor) are conducted similarly to the above. An appropriate cell lysate or purified NHR is used as the source of the NHR. The fluorescent probe and unlabeled competitor are appropriate for the specific NHR, i.e., are ligands for the specific NHR.
- ChEMBL_1658413 (CHEMBL1247284) Antagonist activity at GAL4-fused human GR LBD (443 to 777 residues) expressed in CHO-K1 cells assessed as inhibition of dexamethasone-induced transactivation activity after 5 to 6 hrs by luciferase reporter gene assay
- ChEMBL_1630548 (CHEMBL1108262) Competitive inhibition of His6-tagged human liver glycogen phosphorylase-a expressed in Escherichia coli BL21 Gold (DE3) assessed as release of inorganic phosphate using varying levels of glucose-1-phosphate and constant concentration of AMP and glycogen measured after 1 min by Dixon plot method