Target (1)
Compound (42)
Article Title (328)
Article Author (1)
Assay (615)
(4-{3-[1-(3-Aminomethyl-benzylcarbamoyl)-3-methyl-butylcarbamoyl]-1-cyclohexylmethyl-2-hydroxy-propylcarbamoyl}-1-benzyl-butyl)-carbamic acid tert-butyl ester : (0.6 chloroform) CHEMBL352450 BDBM50016037
BDBM50016040 CHEMBL435076 {1-Benzyl-4-[3-(1-benzylcarbamoyl-3-methyl-butylcarbamoyl)-1-cyclohexylmethyl-2-hydroxy-propylcarbamoyl]-but-2-enyl}-carbamic acid tert-butyl ester : (0.1 chloroform)
BDBM50016060 {1-Benzyl-4-[1-benzyl-3-(1-benzylcarbamoyl-3-methyl-butylcarbamoyl)-2-hydroxy-propylcarbamoyl]-but-2-enyl}-carbamic acid tert-butyl ester : (0.2 chloroform) CHEMBL168819
CHEMBL167204 (1-Benzyl-4-{1-[2-(1-benzylcarbamoyl-3-methyl-butylcarbamoyl)-1-hydroxy-ethyl]-3-methyl-butylcarbamoyl}-butyl)-carbamic acid tert-butyl ester : (0.2 chloroform) BDBM50016041
{1-Benzyl-4-[3-(1-benzylcarbamoyl-3-methyl-butylcarbamoyl)-1-cyclohexylmethyl-2-hydroxy-propylcarbamoyl]-2-hydroxy-butyl}-carbamic acid tert-butyl ester : (0.45 chloroform) BDBM50016025 CHEMBL354821
[1-(3-{[3-(1-Benzylcarbamoyl-3-methyl-butylcarbamoyl)-1-cyclohexylmethyl-2-hydroxy-propylcarbamoyl]-methyl}-oxiranyl)-2-phenyl-ethyl]-carbamic acid tert-butyl ester : (0.7 chloroform) BDBM50016032 CHEMBL353204
(1-Benzyl-4-{1-[2-(1-benzylcarbamoyl-3-methyl-butylcarbamoyl)-1-hydroxy-ethyl]-3-methyl-butylcarbamoyl}-2,3,4-trihydroxy-butyl)-carbamic acid tert-butyl ester : (0.25 chloroform) CHEMBL354147 BDBM50016031
(4-{3-[1-(4-Aminomethyl-benzylcarbamoyl)-3-methyl-butylcarbamoyl]-1-cyclohexylmethyl-2-hydroxy-propylcarbamoyl}-1-benzyl-2-hydroxy-butyl)-carbamic acid tert-butyl ester : (0.5 chloroform) BDBM50016034 CHEMBL423262
CHEMBL168302 (4-{1-[2-(1-Benzylcarbamoyl-3-methyl-butylcarbamoyl)-1-hydroxy-ethyl]-3-methyl-butylcarbamoyl}-1-cyclohexylmethyl-2,3-dihydroxy-butyl)-carbamic acid tert-butyl ester : (0.25 chloroform) BDBM50016054
CHEMBL350359 BDBM50016027 3-Hydroxy-6-methyl-4-(2-{3-[1-(3-methyl-butyrylamino)-2-phenyl-ethyl]-oxiranyl}-acetylamino)-heptanoic acid (1-benzylcarbamoyl-3-methyl-butyl)-amide : (0.1 chloroform)
CHEMBL354969 (1-Benzyl-4-{1-[2-(1-benzylcarbamoyl-3-methyl-butylcarbamoyl)-1-hydroxy-ethyl]-3-methyl-butylcarbamoyl}-2,3-dihydroxy-butyl)-carbamic acid tert-butyl ester : (0.3 chloroform) BDBM50016066
{1-Benzyl-4-[3-(1-benzylcarbamoyl-3-methyl-butylcarbamoyl)-1-cyclohexylmethyl-2-hydroxy-propylcarbamoyl]-2-hydroxy-but-3-enyl}-carbamic acid tert-butyl ester : (0.25 chloroform) CHEMBL167426 BDBM50016046
CHEMBL167218 {1-[3-({3-[1-(3-Aminomethyl-benzylcarbamoyl)-3-methyl-butylcarbamoyl]-1-cyclohexylmethyl-2-hydroxy-propylcarbamoyl}-methyl)-oxiranyl]-2-phenyl-ethyl}-carbamic acid tert-butyl ester : (0.9 chloroform) BDBM50016042
CHEMBL424536 (4-{1-[2-(1-Benzylcarbamoyl-3-methyl-butylcarbamoyl)-1-hydroxy-ethyl]-3-methyl-butylcarbamoyl}-1-isobutyl-2-oxo-5-phenyl-pentyl)-carbamic acid benzyl ester : (0.05 chloroform) BDBM50016057
BDBM50016067 [1-Benzyl-4-(3-{1-[4-(benzyloxycarbonylamino-methyl)-benzylcarbamoyl]-3-methyl-butylcarbamoyl}-1-cyclohexylmethyl-2-hydroxy-propylcarbamoyl)-2-hydroxy-but-3-enyl]-carbamic acid tert-butyl ester : (0.45 chloroform) CHEMBL435266
{1-Benzyl-2-[1-[1-benzyl-3-(1-benzylcarbamoyl-3-methyl-butylcarbamoyl)-2-hydroxy-propylcarbamoyl]-2-(1H-imidazol-4-yl)-ethylamino]-ethyl}-carbamic acid tert-butyl ester : (0.2 chloroform) BDBM50016021 CHEMBL354767
{1-Benzyl-2-[1-{1-[2-(1-benzylcarbamoyl-3-methyl-butylcarbamoyl)-1-hydroxy-ethyl]-3-methyl-butylcarbamoyl}-2-(1H-imidazol-4-yl)-ethylamino]-ethyl}-carbamic acid tert-butyl ester : (0.07 chloroform) CHEMBL168261 BDBM50016056
Phosphinic Peptide Inhibitor, 28 FII 2-benzyl-3-{[1-(2-acetamido-4-methylpentanoyl)pyrrolidin-2-yl](hydroxy)phosphoryl}propanoic acid The second fraction of the HPLC chromatogram. BDBM21464
BDBM567799 US11420968, Example 8 from CN106749233A
BDBM362180 US10272077, Example 8 from US 2010/0179166 US9833448, Example 10 from U.S. Pat. No. 7,390,798
US9833448, Example 8 from US 2010/0179166 BDBM362181 US10272077, Example 32 from U.S. Pat. No. 7,390,798
BDBM362178 US9833448, Example 8 from U.S. Pat. No. 7,390,798 US10272077, Example 8 from U.S. Pat. No. 7,390,798
BDBM362179 US10272077, Example 9 from U.S. Pat. No. 7,390,798 US9833448, Example 9 from U.S. Pat. No. 7,390,798
2-benzyl-3-({1-[2-acetamido-3-(1H-imidazol-4-yl)propanoyl]pyrrolidin-2-yl}(hydroxy)phosphoryl)propanoic acid Phosphinic Peptide Inhibitor, 34 FII The second fraction of the HPLC chromatogram. BDBM21470
4-Chloro-1-ethyl-5-(4-methoxy-6-((2-(trifluoromethyl)cyclohexyl)amino)pyridin-3-yl)-N-(((1r,4r)-4-(methylsulfonyl)cyclohexyl)methyl)-1H-pyrazole-3-carboxamide, Fraction A US10975057, Example 59 BDBM491775
BDBM491776 4-Chloro-1-ethyl-5-(4-methoxy-6-((2-(trifluoromethyl)cyclohexyl)amino)pyridin-3-yl)-N-(((1r,4r)-4-(methylsulfonyl)cyclohexyl)methyl)-1H-pyrazole-3-carboxamide, Fraction B US10975057, Example 60
BDBM491777 US10975057, Example 61 4-Chloro-1-ethyl-5-(4-methoxy-6-((3-(trifluoromethyl)cyclohexyl)amino)pyridin-3-yl)-N-(((1r,4r)-4-(methylsulfonyl)cyclohexyl)methyl)-1H-pyrazole-3-carboxamide, Fraction A
BDBM491778 US10975057, Example 62 4-Chloro-1-ethyl-5-(4-methoxy-6-((3-(trifluoromethyl)cyclohexyl)amino)pyridin-3-yl)-N-(((1r,4r)-4-(methylsulfonyl)cyclohexyl)methyl)-1H-pyrazole-3-carboxamide, Fraction B
BDBM491786 4-Chloro-1-ethyl-5-(4-methoxy-6-((2-(trifluoromethyl)cyclobutyl)amino)pyridin-3-yl)-N-(((1r,4r)-4-(methylsulfonyl)cyclohexyl)methyl)-1H-pyrazole-3-carboxamide, Fraction B US10975057, Example 72
US10975057, Example 77 BDBM491789 4-Chloro-1-ethyl-5-(4-methoxy-6-((2-(trifluoromethyl)cyclopropyl)amino)pyridin-3-yl)-N-(((1r,4r)-4-(methylsulfonyl)cyclohexyl)methyl)-1H-pyrazole-3-carboxamide, Fraction A
US10975057, Example 78 4-Chloro-1-ethyl-5-(4-methoxy-6-((2-(trifluoromethyl)cyclopropyl)amino)pyridin-3-yl)-N-(((1r,4r)-4-(methylsulfonyl)cyclohexyl)methyl)-1H-pyrazole-3-carboxamide, Fraction B BDBM491790
BDBM621058 US20230303556, Example 89 from WO2021/055744
BDBM621059 US20230303556, Example 102 from WO2021/055744
BDBM621060 US20230303556, Example 24 from WO2021/055744
BDBM621061 US20230303556, Example 43 from WO2021/055744
BDBM621063 US20230303556, Example 83 from WO2021/055744
US20230303556, Example 35 from WO2021/055744 BDBM621062
US20230303556, Example 82 from WO2021/055744 BDBM621056
US20230303556, Example 88 from WO2021/055744 BDBM621057
3-{[1-(2-acetamido-4-methylpentanoyl)pyrrolidin-2-yl](hydroxy)phosphoryl}-2-[(3-phenyl-1,2-oxazol-5-yl)methyl]propanoic acid The second fraction of the HPLC chromatogram. BDBM21473 Phosphinic Peptide Inhibitor, 40 FII
BDBM491785 4-Chloro-1-ethyl-5-(4-methoxy-6-((2-(trifluoromethyl)cyclobutyl)amino)pyridin-3-yl)-N-(((1r,4r)-4-(methylsulfonyl)cyclohexyl)methyl)-1H-pyrazole-3-carboxamide, Fraction A US10975057, Example 72 US10975057, Example 71
US20240199576, Example Table 3 from WO 2016/049165 (isomer 1) BDBM681440 US20240199576, Example Table 3 from WO 2016/049165 (isomer 2)
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ChEMBL_763592 (CHEMBL1820033) Displacement of [3H]PK11195 from TSPO in rat kidney mitochondrial fraction
ChEMBL_763593 (CHEMBL1820034) Displacement of [3H]PK11195 from TSPO in human HEK293 mitochondrial fraction
ChEBML_211949 Inhibition of Tripeptidyl-peptidase II purified from a rat liver post-lysosomal fraction.
ChEMBL_211945 (CHEMBL816535) Inhibition of Tripeptidyl-peptidase II purified from a rat liver post-lysosomal fraction.
ChEMBL_424403 (CHEMBL911334) Displacement of [3H]DAMGO from mu opioid receptor in rat synaptosomes P2 fraction
ChEMBL_424404 (CHEMBL911335) Displacement of [3H]deltorphin II from delta opioid receptor in rat synaptosomes P2 fraction
ChEMBL_430079 (CHEMBL918101) Displacement of [3H]DPDPE from delta opioid receptor in rat brain synaptosomes P2 fraction
ChEMBL_430080 (CHEMBL918102) Displacement of [3H]DAMGO from mu opioid receptor in rat brain synaptosomes P2 fraction
ChEMBL_1499884 (CHEMBL3583216) Displacement of [3H]-dexamethasone from cytosolic fraction of human recombinant glucocorticoid receptor by scintillation counting analysis
ChEMBL_1499890 (CHEMBL3583484) Displacement of [3H]-aldosterone from cytosolic fraction of human recombinant mineralocorticoid receptor by scintillation counting analysis
ChEBML_159280 In vitro inhibitory activity against prostaglandin G/H synthase 1 from the microsomal fraction of ram seminal vesicles
ChEMBL_1499885 (CHEMBL3583217) Displacement of [3H]-progesterone from cytosolic fraction of human recombinant progesterone-B receptor by scintillation counting analysis
ChEMBL_2261405 (CHEMBL5216416) Displacement of [14C]-ethanolamine from FAAH derived from rat brain membrane fraction preincubated for 20 mins followed by susbstrate addition by scintillation counting method
ChEMBL_940036 (CHEMBL2327845) Displacement of DAGO from MOR in guinea pig brain membrane fraction after 30 mins by scintillation counting analysis
ChEBML_156450 Inhibition of bovine cardiac phosphodiesterase fraction III
ChEBML_58162 Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEBML_155549 Inhibition of fraction II of guinea pig phosphodiesterase
ChEBML_176345 Inhibition of dopamine uptake in rat synaptosomal fraction
ChEBML_176350 Inhibition of noradrenaline uptake in rat synaptosomal fraction
ChEBML_58396 Displacement of [3H]YM-09151-2 (60 pm) from dopamine receptor D2 in crude membrane fraction of rat brain corpus striatum
ChEMBL_1658426 (CHEMBL4008038) Displacement of [3H]-Aldosterone from MR in rat kidney cytosolic fraction measured after 18 hrs by liquid scintillation counting method
ChEMBL_940038 (CHEMBL2327847) Displacement of [3H]Cl-977 from KOR in guinea pig brain membrane fraction after 30 mins by scintillation counting analysis
ChEMBL_1499893 (CHEMBL3583487) Displacement of [3H]methyltrienolone from cytosolic fraction of androgen receptor in human LANCAP cells after 24 hrs by scintillation counting analysis
ChEBML_176338 Inhibition of 5-HT uptake in rat synaptosomal fraction
ChEMBL_155544 (CHEMBL759912) Inhibition of fraction I of guinea pig phosphodiesterase
ChEMBL_155561 (CHEMBL762673) Inhibition of fraction III of guinea pig phosphodiesterase
ChEMBL_176345 (CHEMBL783267) Inhibition of dopamine uptake in rat synaptosomal fraction
ChEMBL_176350 (CHEMBL781943) Inhibition of noradrenaline uptake in rat synaptosomal fraction
ChEMBL_1463279 (CHEMBL3399468) Displacement of [3H]MPPF from 5HT1A receptor in Sprague-Dawley rat hippocampal membrane fraction incubated for 60 mins by scintillation counting method
ChEMBL_1572346 (CHEMBL3795929) Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL_1658427 (CHEMBL4008039) Displacement of [3H]-Aldosterone from MR in Sprague-Dawley rat kidney cytosolic fraction measured after overnight incubation by liquid scintillation counting method
ChEMBL_1461693 (CHEMBL3395231) Inhibition of 11beta-HSD1 in HEK293 cell microsomal fraction
ChEMBL_176338 (CHEMBL784031) Inhibition of 5-HT uptake in rat synaptosomal fraction
ChEMBL_511117 (CHEMBL1001316) Inhibition of human PDE4B1 in cytosolic fraction of lung
ChEMBL_511118 (CHEMBL1001317) Inhibition of human PDE4B1 in particular fraction of lung
ChEMBL_511119 (CHEMBL1001318) Inhibition of human PDE4B2 in cytosolic fraction of lung
ChEMBL_511120 (CHEMBL1001319) Inhibition of human PDE4B2 in particular fraction of lung
ChEMBL_511121 (CHEMBL1001321) Inhibition of human PDE4B3 in cytosolic fraction of lung
ChEMBL_511122 (CHEMBL1001322) Inhibition of human PDE4B3 in particular fraction of lung
ChEMBL_511124 (CHEMBL999595) Inhibition of human PDE4D1 in cytosolic fraction of lung
ChEMBL_511125 (CHEMBL999596) Inhibition of human PDE4D2 in cytosolic fraction of lung
ChEMBL_511126 (CHEMBL999597) Inhibition of human PDE4D3 in cytosolic fraction of lung
ChEMBL_511127 (CHEMBL999598) Inhibition of human PDE4D3 in particular fraction of lung
ChEMBL_511128 (CHEMBL999599) Inhibition of human PDE4D4 in cytosolic fraction of lung
ChEMBL_511129 (CHEMBL999600) Inhibition of human PDE4D4 in particular fraction of lung
ChEMBL_511130 (CHEMBL999601) Inhibition of human PDE4D5 in cytosolic fraction of lung
ChEMBL_511131 (CHEMBL999602) Inhibition of human PDE4D5 in particular fraction of lung
ChEMBL_1795802 (CHEMBL4267919) Displacement of [3H]DTG from S1R in P2 fraction of Hartley guinea pig whole brain after 90 mins by liquid scintillation counting method
ChEMBL_141416 (CHEMBL752320) Displacement of [3H]ifendropil from binding site of N-methyl-D-aspartate glutamate receptor was evaluated employing synaptosomal fraction of porcine hippocampal brain membranes
ChEMBL_155552 (CHEMBL759850) Inhibition of phosphodiesterase fraction III in anesthetized open chest dogs
ChEMBL_155556 (CHEMBL760020) Inhibition of phosphodiesterase fraction III in anesthetized open chest dogs
ChEMBL_1358464 (CHEMBL3281632) Displacement of 1 x 10'-8 M of [1,2,3-3H]-triamcinolone acetonide from glucocorticoid receptor in soluble fraction of mouse L929 cells after 20 hrs
ChEMBL_1358466 (CHEMBL3281634) Displacement of 2 x 10'-8 M of [1,2,3-3H]-triamcinolone acetonide from glucocorticoid receptor in soluble fraction of mouse L929 cells after 20 hrs
ChEMBL_1658402 (CHEMBL4008014) Displacement of [3H]-Aldosterone from MR in rat renal soluble fraction measured after 18 hrs in presence of glucocorticoid receptor antagonist RU-486 by liquid scintillation counting method
ChEMBL_1904878 (CHEMBL4407236) Inhibition of 17beta-HSD3 in Sprague-Dawley rat testes microsomal fraction assessed as reduction in [14C]-testosterone formation from [14C]-4-androstene-3,17-dione measured after 2 hrs
ChEBML_161419 Kinetic constant was measured for PMII of Leishmania donovani promastigotes using supernatant (S12) fraction
ChEMBL_539041 (CHEMBL1035715) Inhibition of HO1 in rat spleen microsomal fraction assessed as carbon monoxide production
ChEMBL_1474762 (CHEMBL3424219) Inhibition of human 11beta-HSD1 overexpressed in microsomal fraction of HEK293 cells assessed as formation of [3H]-cortisol from [3H]-cortisone by scintillation proximity assay in presence of NADPH
ChEMBL_1474764 (CHEMBL3424221) Inhibition of mouse 11beta-HSD1 overexpressed in microsomal fraction of HEK293 cells assessed as formation of [3H]-cortisol from [3H]-cortisone by scintillation proximity assay in presence of NADPH
ChEMBL_1453699 (CHEMBL3364101) Inhibition of rat MAO-B in rat-liver mitochondrial-fraction using [14C]-PEA substrate
ChEMBL_161419 (CHEMBL766687) Kinetic constant was measured for PMII of Leishmania donovani promastigotes using supernatant (S12) fraction
ChEMBL_216037 (CHEMBL819744) Evaluated for beta-receptor affinity determined in rat brain membrane fraction with [3H]- dihydroalprenolol
ChEMBL_216038 (CHEMBL819745) Evaluated for beta-receptor affinity, determined in rat brain membrane fraction with [3H]- dihydroalprenolol
ChEMBL_1798975 (CHEMBL4271267) Inhibition of partially purified HDAC isolated from human M8 cells enzyme fraction pre-incubated for 5 mins before [3H]acetylated histone addition and measured after 30 mins by scintillation counting method
ChEBML_1540144 Inhibition of human MAO-B expressed in baculovirus infected BT1 cells microsome fraction by fluorescence spectrometry
ChEBML_1540145 Inhibition of human MAO-A expressed in baculovirus infected BT1 cells microsome fraction by fluorescence spectrometry
ChEMBL_1453698 (CHEMBL3364100) Inhibition of rat MAO-A in rat-liver mitochondrial-fraction using [14C]-5-HT substrate
ChEMBL_757264 (CHEMBL1803640) Inhibition of ICMT assessed as accumulation of ras in cytosolic fraction by cell based assay
ChEMBL_1540144 (CHEMBL3738353) Inhibition of human MAO-B expressed in baculovirus infected BT1 cells microsome fraction by fluorescence spectrometry
ChEMBL_154395 (CHEMBL759157) Inhibition of canine cardiac fraction III cAMP phosphodiesterase (PDE 3) at 0.875 mg/kg intravenous dose
ChEMBL_154396 (CHEMBL759158) Inhibition of canine cardiac fraction III cAMP phosphodiesterase (PDE 3) at 1.875 mg/kg intravenous dose
ChEMBL_161421 (CHEMBL766689) Kinetic constant was measured for Protein Methylase II of Leishmania donovani promastigotes using supernatant (S12) fraction
ChEMBL_1921322 (CHEMBL4424167) Inhibition of MAO-A in mouse brain mitochondrial fraction using kynuramine as substrate by fluorometric analysis
ChEMBL_154397 (CHEMBL759159) Inhibitory activity against canine cardiac fraction III cyclic AMP phosphodiesterase (PDE III) at 8.75 mg/kg intravenous dose
ChEMBL_2308592 Inhibition of human PDE10A2 transfected in human AD293 cells cytosolic fraction using cAMP as substrate by fluorescence polarization assay
ChEMBL_826632 (CHEMBL2050886) Inhibition of mPGES-1 derived from IL1beta and TNFalpha stimulated human HeLa cells microsomal fraction using PGH2 as substrate preincubated for 30 mins prior to substrate addition measured after 1 min by LC-MS/MS analysis
ChEMBL_1793492 (CHEMBL4265411) Inhibition of RALDH2 in choroidal cytosol fraction from 4 day recovering chick assessed as inhibition of ATRA synthesis pre-incubated for 20 mins followed by ATRA and NAD+ addition and measured after 30 mins by HPLC analysis
ChEMBL_1921320 (CHEMBL4424165) Inhibition of MAO-A in mouse brain mitochondrial fraction using kynuramine as substrate after 30 mins by fluorometric analysis
ChEMBL_1752866 (CHEMBL4187626) Inhibition of human FAAH expressed in baculovirus-infected High Five cells S9 fraction using OMP substrate by fluorescence based assay
ChEMBL_726920 (CHEMBL1686709) Inhibition of mPGES-1 expressed in LPS-stimulated human A549 cells mitochondrial fraction assessed as conversion of PGH2 to PGE2
ChEMBL_1363487 (CHEMBL3291709) Inhibition of human placental 17beta-HSD2 microsomal fraction using tritiated estradiol as substrate assessed as formation of estrone by HPLC analysis
ChEMBL_1363489 (CHEMBL3291711) Inhibition of human placental 17beta-HSD1 cytosolic fraction using tritiated estrone as substrate assessed as formation of estradiol by HPLC analysis
ChEMBL_1363494 (CHEMBL3291985) Inhibition of mouse liver 17beta-HSD2 microsomal fraction using tritiated estradiol as substrate assessed as formation of estrone by HPLC analysis
ChEMBL_1466123 (CHEMBL3404741) Inhibition of human 11beta-HSD1 using microsomal fraction and NADPH assessed as conversion of cortisone to cortisol by biochemical enzyme assay
ChEMBL_1466125 (CHEMBL3404743) Inhibition of mouse 11beta-HSD1 using microsomal fraction and NADPH assessed as conversion of cortisone to cortisol by biochemical enzyme assay
ChEMBL_1466126 (CHEMBL3404744) Inhibition of human 11beta-HSD2 using microsomal fraction and NADPH assessed as conversion of cortisone to cortisol by biochemical enzyme assay
ChEMBL_1541061 (CHEMBL3744292) Inhibition of 17beta-HSD2 in human placental microsomal fraction using E2/NAD+ as substrate/cofactor after 20 mins by HPLC analysis
ChEMBL_1541062 (CHEMBL3744293) Inhibition of 17beta-HSD1 in human placental cytosolic fraction using E1/NADH as substrate/cofactor after 10 mins by HPLC analysis
ChEMBL_1861097 (CHEMBL4361953) Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate in presence of NAD+ by radio-HPLC analysis
ChEMBL_1861098 (CHEMBL4361954) Inhibition of human placental cytosolic fraction 17beta-HSD1 using [3H]-E1 as substrate in presence of NAD+ by radio-HPLC analysis
ChEMBL_1863749 (CHEMBL4364724) Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate in presence of NAD+ by radio-HPLC analysis
ChEMBL_1863752 (CHEMBL4364727) Inhibition of human placental cytosolic fraction 17beta-HSD1 using [3H]-E1 as substrate in presence of NAD+ by radio-HPLC analysis
ChEMBL_1898526 (CHEMBL4400641) Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate in presence of NAD+ by radio-HPLC analysis
ChEMBL_1898527 (CHEMBL4400642) Inhibition of human placental cytosolic fraction 17beta-HSD1 using [3H]-E1 as substrate in presence of NAD+ by radio-HPLC analysis
ChEMBL_1446069 (CHEMBL3380296) Inhibition of human recombinant MDR1 in cell membrane fraction preincubated for 5 mins measured after 40 mins by Pgp-Glo luciferase assay
ChEMBL_606059 (CHEMBL1071958) Inhibition of SCD1 in mouse microsomal liver S9 microsomal fraction assessed as conversion of [14C]stearate to [14C]oleate after 60 mins
ChEMBL_798594 (CHEMBL1942485) Inhibition of alpha-glucosidase activity of maltase in rat small intestinal brush border membrane fraction using maltose as substrate after 30 mins
ChEMBL_798596 (CHEMBL1942487) Inhibition of alpha-glucosidase activity of sucrase in rat small intestinal brush border membrane fraction using maltose as substrate after 30 mins
ChEMBL_938947 (CHEMBL2328436) Inhibition of 17beta-HSD1 in human placental cytosolic fraction using [3H]E1 as substrate assessed as formation of E2 by HPLC analysis
ChEMBL_938948 (CHEMBL2328437) Inhibition of 17beta-HSD2 in human placental microsomal fraction using [3H]E2 as substrate assessed as formation of E1 by HPLC analysis
ChEMBL_1367282 (CHEMBL3300203) Inhibition of human placental 17beta-HSD1 cytosolic fraction using [2, 4, 6, 7-3H]-estrone as substrate after 10 mins by HPLC analysis
ChEMBL_1367283 (CHEMBL3300204) Inhibition of human placental 17beta-HSD2 microsomal fraction using [2, 4, 6, 7-3H]-estradiol as substrate after 20 mins by HPLC analysis
ChEMBL_1752865 (CHEMBL4187625) Inhibition of human recombinant soluble epoxide hydrolase expressed in baculovirus-infected High Five cells S9 fraction using CMNPC substrate by fluorescence based assay
ChEMBL_1849337 (CHEMBL4349878) Inhibition of SOAT1 in CHO cell microsomal fraction using [1-14C]oleoyl-CoA as substrate measured after 5 mins by TLC based method
ChEMBL_1866205 (CHEMBL4367180) Inhibition of isopentenyl diphosphate isomerase in Sprague-Dawley rat liver S100 fraction preincubated for 10 min followed by MVA addition by HPLC analysis
ChEMBL_2324327 Inhibition of human placental cytosolic fraction 17beta-HSD1 using [3H]E1 as substrate measured after 10 mins in presence of NADH by HPLC analysis
ChEMBL_2324328 Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]E2 as substrate measured after 20 mins in presence of NAD+ by HPLC analysis
ChEMBL_736715 (CHEMBL1695096) Inhibition of Prostaglandin E2 synthase-1 in IL1-beta stimulated microsomal fraction of human A549 cell assessed as PGE2 level by RP-HPLC
ChEMBL_1470660 (CHEMBL3420247) Inhibition of HO1 in Sprague-Dawley rat spleen microsomal fraction assessed as reduction in bilirubin formation incubated for 60 mins by double beam spectrophotometry
ChEMBL_1470661 (CHEMBL3420440) Inhibition of HO2 in Sprague-Dawley rat brain microsomal fraction assessed as reduction in bilirubin formation incubated for 60 mins by double beam spectrophotometry
ChEMBL_1702993 (CHEMBL4054226) Inhibition of full-length mouse 11beta-HSD1 expressed in HEK293 microsomal fraction using [3H]cortisone as substrate after 1 hr by scintillation proximity assay
ChEMBL_1702996 (CHEMBL4054229) Inhibition of full-length human 11beta-HSD1 expressed in HEK293 microsomal fraction using [3H]cortisone as substrate after 2 hr by scintillation proximity assay
ChEMBL_1702997 (CHEMBL4054230) Inhibition of full-length mouse 11beta-HSD2 expressed in HEK293 microsomal fraction using [3H]cortisone as substrate after 1 hr by scintillation proximity assay
ChEMBL_1702998 (CHEMBL4054231) Inhibition of full-length human 11beta-HSD2 expressed in HEK293 microsomal fraction using [3H]cortisone as substrate after 2 hr by scintillation proximity assay
ChEMBL_1921326 (CHEMBL4424171) Inhibition of MAO-A in Sprague-Dawley rat brain mitochondrial fraction after 10 mins in presence of [14C]5-hydroxytryptamine by liquid scintillation analysis
ChEMBL_2173334 (CHEMBL5058468) Inhibition of human placental cytosolic fraction 17beta-HSD1 using [3H]-E1 as substrate in presence of NADH measured after 10 mins by HPLC method
ChEMBL_2173335 (CHEMBL5058469) Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate in presence of NAD+ measured after 20 mins by HPLC method
ChEMBL_2217338 (CHEMBL5130470) Inhibition of human placental cytosolic fraction 17beta-HSD1 using [3H]-E1 as substrate in presence of NADH measured after 10 mins by HPLC method
ChEMBL_2217339 (CHEMBL5130471) Inhibition of human placental microsomal fraction 17beta-HS2 using [3H]-E2 as substrate in presence of NAD+ measured after 10 mins by HPLC method
ChEMBL_606061 (CHEMBL1071960) Inhibition of SCD1 in human liver S9 microsomal fraction assessed as conversion of [14C]stearate to [14C]oleate after 60 mins at 0.4 uM
ChEMBL_1474763 (CHEMBL3424220) Inhibition of mouse 11beta-HSD2 overexpressed in microsomal fraction of HEK293 cells using [3H]-cortisol as substrate by scintillation proximity assay in presence of NAD+
ChEMBL_1474766 (CHEMBL3424223) Inhibition of human 11beta-HSD2 overexpressed in microsomal fraction of HEK293 cells using [3H]-cortisol as substrate by scintillation proximity assay in presence of NAD+
ChEMBL_1789617 (CHEMBL4261351) Inhibition of mouse microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate after 20 mins in presence of NAD+ by radio-flow detector based analysis
ChEMBL_606058 (CHEMBL1071957) Inhibition of SCD1 in human 293A cells assessed as conversion of [14C]stearate to [14C]oleate after 60 mins in presence of S9 microsomal fraction
ChEMBL_988473 (CHEMBL2438122) Inhibition of human placenta 17beta-HSD1 cytosolic fraction using unlabeled, [2,4,6,7-3H]-estrone as substrate after 20 mins by HPLC analysis in presence of NADH
ChEMBL_988475 (CHEMBL2438124) Inhibition of human placenta 17beta-HSD2 microsomal fraction using unlabeled, [2,4,6,7-3H]-estradiol as substrate after 20 mins by HPLC analysis in presence of NAD+
ChEBML_31943 Inhibition of aldose reductase from rat lens. Value ranges from 0.07 - 1.2
ChEMBL_72759 (CHEMBL874131) Inhibition of Glutathionylspermidine synthetase from Escherichia coli, value taken from literature
ChEMBL_947924 (CHEMBL2343667) Displacement of [125I]alpha-bungarotoxin from alpha7 nAChR from rat hippocampus
ChEMBL_1752869 (CHEMBL4187629) Competitive inhibition of human recombinant soluble epoxide hydrolase expressed in baculovirus-infected High Five cells S9 fraction using varying CMNPC substrate levels by fluorescence based assay
ChEMBL_1789612 (CHEMBL4261346) Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate after 20 mins in presence of NAD+ by radio-flow detector based analysis
ChEMBL_1882121 (CHEMBL4383620) Inhibition of FAAH in rat liver S9 fraction using N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide as substrate after 60 mins by fluorescence-based HPLC analysis
ChEMBL_1994033 (CHEMBL4627928) Inhibition of human SOAT1-mediated [14C]Cholesterol ester biosynthesis in CHO microsomal fraction after 5 mins in presence of [1-14C]oleoyl-CoA by TLC analysis
ChEMBL_1994034 (CHEMBL4627929) Inhibition of human SOAT2-mediated [14C]Cholesterol ester biosynthesis in CHO microsomal fraction after 5 mins in presence of [1-14C]oleoyl-CoA by TLC analysis
ChEMBL_861317 (CHEMBL2173705) Inhibition of human placenta 17beta-HSD1 cytosolic fraction using unlabelled and [2,4,6,7-3H]estrone as substrate after 10 mins by HPLC analysis in presence of NADH
ChEMBL_861318 (CHEMBL2173706) Inhibition of human placenta 17beta-HSD2 microsomal fraction using unlabelled and [2,4,6,7-3H]estradiol as substrate after 20 mins by HPLC analysis in presence of NAD+
ChEBML_140043 Displacement of [3H]QNB from Muscarinic acetylcholine receptor M2 from rat heart homogenates
ChEBML_212946 Binding affinity to uridine kinase from L1210. was determined from the dixon plot
ChEBML_212947 Binding affinity to uridine kinase from L1210. was determined from the dixon plot
ChEMBL_1659415 (CHEMBL4009027) Displacement of [3H]R21412 from from in Sprague-Dawley rat cerebrocortical membranes
ChEMBL_215167 (CHEMBL821340) Displacement of [3H]AVP from vasopressin receptor (V1a) from human platelet membranes.
ChEMBL_31942 (CHEMBL640404) Inhibition of aldose reductase from rat lens. Value ranges from 0.02 -0.64
ChEMBL_31944 (CHEMBL640406) Inhibition of aldose reductase from rat lens. Value ranges from 0.1 - 7
ChEMBL_31945 (CHEMBL640407) Inhibition of aldose reductase from rat lens. Value ranges from 0.15 - 3.3
ChEMBL_31946 (CHEMBL640408) Inhibition of aldose reductase from rat lens. Value ranges from 0.3 - 2.3
ChEMBL_31947 (CHEMBL640409) Inhibition of aldose reductase from rat lens. Value ranges from 0.5 - 16
ChEMBL_31948 (CHEMBL640410) Inhibition of aldose reductase from rat lens. Value ranges from 0.6 - 47
ChEMBL_31949 (CHEMBL640502) Inhibition of aldose reductase from rat lens. Value ranges from 1.0 - 34
ChEMBL_31950 (CHEMBL640503) Inhibition of aldose reductase from rat lens. Value ranges from 1.5 - 16
ChEMBL_31951 (CHEMBL640504) Inhibition of aldose reductase from rat lens. Value ranges from 10 - 130
ChEMBL_31952 (CHEMBL640505) Inhibition of aldose reductase from rat lens. Value ranges from 10 - 1300
ChEMBL_31953 (CHEMBL640506) Inhibition of aldose reductase from rat lens. Value ranges from 10 - 42
ChEMBL_32067 (CHEMBL645979) Inhibition of aldose reductase from rat lens. Value ranges from 10 - 520
ChEMBL_32068 (CHEMBL645980) Inhibition of aldose reductase from rat lens. Value ranges from 110 - 430
ChEMBL_32069 (CHEMBL884117) Inhibition of aldose reductase from rat lens. Value ranges from 140 - 580
ChEMBL_32070 (CHEMBL645981) Inhibition of aldose reductase from rat lens. Value ranges from 16 - 360
ChEMBL_32071 (CHEMBL645982) Inhibition of aldose reductase from rat lens. Value ranges from 17 - 720
ChEMBL_32072 (CHEMBL645983) Inhibition of aldose reductase from rat lens. Value ranges from 20 - 160
ChEMBL_32073 (CHEMBL645984) Inhibition of aldose reductase from rat lens. Value ranges from 25-64
ChEMBL_32074 (CHEMBL645985) Inhibition of aldose reductase from rat lens. Value ranges from 280 - 490
ChEMBL_32075 (CHEMBL645986) Inhibition of aldose reductase from rat lens. Value ranges from 3 - 300
ChEMBL_32076 (CHEMBL645987) Inhibition of aldose reductase from rat lens. Value ranges from 300 - 1100
ChEMBL_32077 (CHEMBL645988) Inhibition of aldose reductase from rat lens. Value ranges from 300 - 2000
ChEMBL_32078 (CHEMBL645989) Inhibition of aldose reductase from rat lens. Value ranges from 32 - 110
ChEMBL_32079 (CHEMBL643656) Inhibition of aldose reductase from rat lens. Value ranges from 35-160
ChEMBL_32080 (CHEMBL643657) Inhibition of aldose reductase from rat lens. Value ranges from 4.9 - 23
ChEMBL_32081 (CHEMBL643658) Inhibition of aldose reductase from rat lens. Value ranges from 40 - 680
ChEMBL_32082 (CHEMBL643659) Inhibition of aldose reductase from rat lens. Value ranges from 5 - 97
ChEMBL_32083 (CHEMBL643660) Inhibition of aldose reductase from rat lens. Value ranges from 50 - 650
ChEMBL_32084 (CHEMBL643661) Inhibition of aldose reductase from rat lens. Value ranges from 6 - 14
ChEMBL_32085 (CHEMBL643662) Inhibition of aldose reductase from rat lens. Value ranges from 7 - 130
ChEMBL_32086 (CHEMBL876584) Inhibition of aldose reductase from rat lens. Value ranges from 7 - 33
ChEMBL_32087 (CHEMBL643663) Inhibition of aldose reductase from rat lens. Value ranges from 8.5 - 410
ChEMBL_32088 (CHEMBL643664) Inhibition of aldose reductase from rat lens. Value ranges from 9 - 69
ChEMBL_755707 (CHEMBL1803209) Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL_757942 (CHEMBL1809359) Displacement of [125I]CCK from gastrin receptor isolated from human tumor tissues
ChEMBL_757944 (CHEMBL1809361) Displacement of [125I]CCK from CCK1 receptor isolated from human tumor tissues
Binding Assay Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL_1866206 (CHEMBL4367181) Inhibition of farnesyl diphosphate synthase in Sprague-Dawley rat liver S100 fraction using MVA as substrate preincubated for 10 min followed by MVA addition by HPLC analysis
ChEMBL_1907 (CHEMBL884529) Displacement of [3H]ketanserin from 5-hydroxytryptamine 2 receptor from rat cortical membranes.
ChEMBL_215168 (CHEMBL821341) Displacement of (Phe-3,4,5-H) Vasopressin from V1a receptor from rat liver membranes.
ChEMBL_217679 (CHEMBL819973) Displacement of [3H]nitrendipine from calcium channel receptors (CCRs) from rat cortex homogenate
ChEMBL_29459 (CHEMBL642188) Displacement of [3H]N6-PIA from Adenosine A1 receptor from rat whole brain
ChEMBL_31852 (CHEMBL646639) Displacement of [125I]AB-MECA from adenosine A3 receptor from HEK293 cell membranes
ChEMBL_332070 (CHEMBL859602) Displacement of [3H]GR65630 from 5HT3 receptor in brain cortex from Wistar rat
ChEMBL_442251 (CHEMBL892410) Displacement of [3H]PIB from beta amyloid in brain homogenate from Alzheimer's patient
ChEMBL_456104 (CHEMBL888113) Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL_456105 (CHEMBL888114) Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
ChEMBL_766140 (CHEMBL1826107) Displacement of [3H]-pentazocine from sigma 1 receptor from guinea pig brain membrane
ChEMBL_1274566 (CHEMBL3091166) Inhibition of 17beta-HSD3 in rat testes microsomal fraction using [14C]-4-androstene-3,17-dione as substrate assessed as testosterone formation after 2 hrs by thin layer chromatography
ChEMBL_141414 (CHEMBL751708) Compound was tested for inhibition of [3H]MK-801 binding to N-methyl-D-aspartate glutamate receptor at NR2B subunit in high affinity fraction of porcine brain membranes
ChEMBL_141415 (CHEMBL751709) Compound was tested for inhibition of [3H]MK-801 binding to N-methyl-D-aspartate glutamate receptor lacking NR2B subunit in low affinity fraction of porcine brain membranes
ChEMBL_2308606 Displacement of MK499 from hERG
ChEBML_28992 Displacement of [3H]CHA from Adenosine A1 receptor of rat forebrain membranes (shielded from light)
ChEBML_48442 Ability to displace [125I]CCK-8 from gastrin/Cholecystokinin type B receptor from rat brain
ChEBML_71109 Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 150-220 nM
ChEMBL_33561 (CHEMBL648423) Displacement of [3H]prazosin from alpha-1 adrenergic receptor from rat brain cerebral cortex
ChEMBL_33764 (CHEMBL650237) Displacement of [3H]idazoxan from alpha-2 adrenergic receptor from rat brain cerebral cortex.
ChEMBL_38284 (CHEMBL647667) Concentration effective against displacing [3H]dihydroalprenolol from beta adrenergic receptor from canine ventricular tissue
ChEMBL_685426 (CHEMBL1285325) Displacement of [3H]N-R-methylhistamine from human H3 receptor isolated from C6 cells
ChEMBL_1796598 (CHEMBL4268715) Inhibition of heme oxygenase 1 in Sprague-Dawley rat spleen microsomal fraction assessed as decrease in bilirubin formation using biliverdin reductase as substrate after 60 mins by spectrophotometric method
ChEBML_146550 The ability to displace [3H]-naloxone from the Opioid receptor mu isolated from rat brain membrane.
ChEBML_30920 Displacement of [3H]-CGS- 21680 from Adenosine A2a receptor of rat forebrain membranes (shielded from light)
ChEBML_54063 Inhibition measurement of orotate formation from radiolabeled dihydroorotate, using partially purified DHODase isolated from human liver.
ChEMBL_2479341 Displacement of [3H]-DAMGO from human MOR extracted from HEK293 cell membrane assessed as inhibition constant
ChEMBL_2479342 Displacement of [3H]DPDPE from human DOR extracted from HEK293 cell membrane assessed as inhibition constant
ChEMBL_28992 (CHEMBL645016) Displacement of [3H]CHA from Adenosine A1 receptor of rat forebrain membranes (shielded from light)
ChEMBL_36341 (CHEMBL650168) Displacement of [3H]-AII from the Angiotensin II receptor isolated from the liver of rats
ChEMBL_48442 (CHEMBL662107) Ability to displace [125I]CCK-8 from gastrin/Cholecystokinin type B receptor from rat brain
ChEMBL_71102 (CHEMBL679614) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 10-12 nM
ChEMBL_71103 (CHEMBL679615) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 106-131 nM
ChEMBL_71104 (CHEMBL679616) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 1273-2947 nM
ChEMBL_71105 (CHEMBL679617) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 13-26 nM
ChEMBL_71106 (CHEMBL679618) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 133-161 nM
ChEMBL_71107 (CHEMBL679619) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 1382-1049 nM
ChEMBL_71108 (CHEMBL679620) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 1428-1433 nM
ChEMBL_71109 (CHEMBL686057) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 150-220 nM
ChEMBL_71110 (CHEMBL686058) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 159-161 nM
ChEMBL_71111 (CHEMBL686059) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 17-21 nM
ChEMBL_71112 (CHEMBL686060) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 2-2 nM
ChEMBL_71113 (CHEMBL686061) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 215-217 nM
ChEMBL_71114 (CHEMBL686295) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 23-33 nM
ChEMBL_71115 (CHEMBL686296) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 26-67 nM
ChEMBL_71116 (CHEMBL686297) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 28-34 nM
ChEMBL_71117 (CHEMBL686298) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 294-554 nM
ChEMBL_71118 (CHEMBL686299) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 3-3 nM
ChEMBL_71228 (CHEMBL682527) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 3-4 nM
ChEMBL_71229 (CHEMBL682528) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 366-578 nM
ChEMBL_71230 (CHEMBL682529) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 378-814 nM
ChEMBL_71231 (CHEMBL682530) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 379-840 nM
ChEMBL_71232 (CHEMBL680299) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 39-94 nM
ChEMBL_71233 (CHEMBL680300) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 43-50 nM
ChEMBL_71234 (CHEMBL680301) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 44-53 nM
ChEMBL_71235 (CHEMBL680302) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 5-6 nM
ChEMBL_71236 (CHEMBL680303) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 536-560 nM
ChEMBL_71237 (CHEMBL680304) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 559-1423 nM
ChEMBL_71238 (CHEMBL680305) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 6-7 nM
ChEMBL_71239 (CHEMBL680306) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 6-8 nM
ChEMBL_71240 (CHEMBL680307) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 61-63 nM
ChEMBL_71241 (CHEMBL680308) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 639-673 nM
ChEMBL_71242 (CHEMBL683338) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 681-974 nM
ChEMBL_71243 (CHEMBL683339) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 70-92 nM
ChEMBL_71244 (CHEMBL683340) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 838-988 nM
ChEMBL_71245 (CHEMBL683341) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 9-12 nM
ChEMBL_71246 (CHEMBL683342) Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR); Value ranges from 949-1169 nM
ChEMBL_822859 (CHEMBL2037891) Displacement of [3H]A585539 from alpha7 nAChR from rat brain membrane with no cerebellum/cortex
ChEMBL_1856724 (CHEMBL4357453) Inhibition of human BK alpha/beta4 channel expressed in HEK293T cells assessed as inhibition of K+ outward current fraction at -80 mV holding potential by whole cell patch clamp technique
ChEMBL_2018315 (CHEMBL4671893) Inhibition of FP-Rh binding to ABHD6 in mouse brain cytosolic fraction preincubated for 1 hr followed by FP-Rh addition and measured after 1 hr by SDS-PAGE analysis
ChEBML_155203 Inhibition of PDE5 from human platelets
ChEMBL_154563 (CHEMBL757898) Inhibition of PDE5 from platelets
ChEMBL_154564 (CHEMBL757899) Inhibition of PDE5 from platelets
ChEMBL_2279433 Displacement of MK499 from human ERG
ChEMBL_30986 (CHEMBL645178) Dissociation constant from Alcohol dehydrogenase
ChEMBL_458742 (CHEMBL943026) Displacement of dofetilide from hERG
ChEMBL_512427 (CHEMBL980768) Displacement of radioligand from NET
ChEMBL_512431 (CHEMBL980772) Displacement of radioligand from DAT
ChEMBL_512438 (CHEMBL980779) Displacement of radioligand from SERT
ChEMBL_622268 (CHEMBL1110413) Displacement of ARC583 from ROCK2
ChEBML_148701 The ability to displace [3H]naloxone from the Opioid receptor mu 1 isolated from rat brain membrane.
ChEBML_148837 Ability to displace [3H]naloxone from the Opioid receptor mu 1 isolated from the rat brain membranes.
ChEBML_58717 Compound was tested for the displacement of [3H]spiperone from Dopamine receptor D2 from rat striatal membranes.
ChEMBL_1286966 (CHEMBL3111131) Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL_143174 (CHEMBL748050) Tested for displacement of radioligand [3H]-Naloxone from opiate receptor; value ranges from 7-10 uM
ChEMBL_143863 (CHEMBL750612) Inhibition of [3H]epibatidine binding to alpha4-beta2 nACh receptor from rat membranes from ref 16
ChEMBL_143870 (CHEMBL751226) Inhibition of [3H]nicotine binding to alpha4-beta2 nACh receptor from rat membranes from ref 14
ChEMBL_143871 (CHEMBL751227) Inhibition of [3H]nicotine binding to alpha4-beta2 nACh receptor from rat membranes from ref 16
ChEMBL_146550 (CHEMBL754969) The ability to displace [3H]-naloxone from the Opioid receptor mu isolated from rat brain membrane.
ChEMBL_146552 (CHEMBL754970) The ability to displace [3H]naloxone from the opioid receptor mu isolated from rat brain membrane.
ChEMBL_157618 (CHEMBL766388) In vitro inhibitory activity against prolyl oligopeptidase (POP) from pig brain; value ranges from (1.1-2.2)
ChEMBL_157619 (CHEMBL766389) In vitro inhibitory activity against prolyl oligopeptidase (POP) from pig brain; value ranges from (1.9-2.5)
ChEMBL_157620 (CHEMBL766917) In vitro inhibitory activity against prolyl oligopeptidase (POP) from pig brain; value ranges from (12-14)
ChEMBL_157621 (CHEMBL766918) In vitro inhibitory activity against prolyl oligopeptidase (POP) from pig brain; value ranges from (21-32)
ChEMBL_157622 (CHEMBL766919) In vitro inhibitory activity against prolyl oligopeptidase (POP) from pig brain; value ranges from (38-110)
ChEMBL_157623 (CHEMBL766920) In vitro inhibitory activity against prolyl oligopeptidase (POP) from pig brain; value ranges from (38-62)
ChEMBL_157624 (CHEMBL766921) In vitro inhibitory activity against prolyl oligopeptidase (POP) from pig brain; value ranges from (44-110)
ChEMBL_157625 (CHEMBL766922) In vitro inhibitory activity against prolyl oligopeptidase (POP) from pig brain; value ranges from (59 - 100)
ChEMBL_157626 (CHEMBL766923) In vitro inhibitory activity against prolyl oligopeptidase (POP) from pig brain; value ranges from (72-92)
ChEMBL_157627 (CHEMBL766924) In vitro inhibitory activity against prolyl oligopeptidase (POP) from pig brain; value ranges from (7800-54000)
ChEMBL_209380 (CHEMBL857872) Binding affinity by displacement of radiolabeled GR-100679 from Tachykinin receptor 2 from homogenized rat colon
ChEMBL_223088 (CHEMBL841331) Inhibition of [3H]nicotine binding to alpha4-beta2 nACh receptor from rat membranes from ref 15
ChEMBL_223089 (CHEMBL841332) Inhibition of [3H]nicotine binding to alpha4-beta2 nACh receptor from rat membranes from ref 18
ChEMBL_223090 (CHEMBL841333) inhibition of [3H]nicotine binding to alpha4-beta2 nACh receptor from rat membranes from ref 18
ChEMBL_2263959 Displacement of [3H]CHA from adenosine A1 receptor derived from rat brain membrane assessed as inhibition constant
ChEMBL_2479343 Displacement of [3H]U-69593 from human KOR extracted from HEK293 cell membrane assessed as inhibition constant
ChEMBL_28018 (CHEMBL641217) In vitro inhibitory concentration against ACAT derived from smooth muscle cells from thoracic aorta of monkeys
ChEMBL_30920 (CHEMBL647730) Displacement of [3H]-CGS- 21680 from Adenosine A2a receptor of rat forebrain membranes (shielded from light)
ChEMBL_630233 (CHEMBL1105635) Displacement of [3H]DAMGO from mu opioid receptor from Wistar rat brain by liquid scintillation counting
ChEMBL_63500 (CHEMBL676491) Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL_65135 (CHEMBL677470) Inhibitory concentration compound against EFGR tyrosine kinase obtained from plasma membrane vesicles from cultured A431 cells
ChEMBL_1337889 (CHEMBL3240916) Inhibition of CYP3A4 in human liver microsomal fraction assessed as midazolam-1'-hydroxylation preincubated for 10 mins followed by NADPH addition measured after 5 to 20 mins by RF-MS analysis
ChEMBL_1337890 (CHEMBL3240917) Inhibition of CYP2C9 in human liver microsomal fraction assessed as diclofenac-4'-hydroxylation preincubated for 10 mins followed by NADPH addition measured after 5 to 20 mins by RF-MS analysis
ChEMBL_1337891 (CHEMBL3240918) Inhibition of CYP2D6 in human liver microsomal fraction assessed as dextromethorphan O-demethylase preincubated for 10 mins followed by NADPH addition measured after 5 to 20 mins by RF-MS analysis
ChEMBL_2244526 (CHEMBL5158736) Inhibition of human recombinant LTC4S expressed in HEK293 cell microsomal fraction preincubated for 10 mins followed by LTA4-methyl ester addition and measured after 10 mins by UPLC-MS/MS analysis
ChEMBL_956682 (CHEMBL2379079) Inhibition of MAGL (unknown origin) expressed in African green monkey COS7 cell cytosolic fraction assessed as [3H]2-AG hydrolysis to [3H]arachidonic acid after 20 mins by beta counting analysis
ChEMBL_143862 (CHEMBL748866) Inhibition of [3H]epibatidine binding to Nicotinic acetylcholine receptor alpha4-beta2 from rat membranes from ref 16
ChEMBL_143865 (CHEMBL750614) Inhibition of [3H]nicotine binding to Nicotinic acetylcholine receptor alpha4-beta2 from rat membranes from ref 14
ChEMBL_148701 (CHEMBL751073) The ability to displace [3H]naloxone from the Opioid receptor mu 1 isolated from rat brain membrane.
ChEMBL_148837 (CHEMBL753955) Ability to displace [3H]naloxone from the Opioid receptor mu 1 isolated from the rat brain membranes.
ChEMBL_1804555 (CHEMBL4303779) hERG binding assays: Displacement of [3H]-Dofetilide (5 nM final) from hERG membranes obtained from HEK293 cells
ChEMBL_2228779 (CHEMBL5142292) Displacement of 125I-labeled angiotensin I from from human plasma renin by gamma counter based competitive radioimmunoassay
ChEMBL_223087 (CHEMBL841330) Inhibition of [3H]nicotine binding to Nicotinic acetylcholine receptor alpha4-beta2 from rat membranes from ref 15
ChEMBL_2263963 Displacement of [3H]cyclohexyladen from A1 adenosine receptor derived from rat cerebral cortical membrane assessed as inhibition constant
ChEMBL_2480421 Displacement of [3H]-raclopride from human D2L receptor extracted from HEK293 cell membrane by microbeta plate reader analysis
ChEMBL_27595 (CHEMBL644315) Displacement of [3H]DPCPX from human Adenosine A1 receptor expressed in CHO cells; ranges from 1460-2201
ChEMBL_27596 (CHEMBL644316) Displacement of [3H]DPCPX from human Adenosine A1 receptor expressed in CHO cells; ranges from 9038-9773
ChEMBL_27597 (CHEMBL644317) Displacement of [3H]-DPCPX from human Adenosine A1 receptor expressed in CHO cells; ranges from 107-181
ChEMBL_27598 (CHEMBL644318) Displacement of [3H]DPCPX from human Adenosine A1 receptor expressed in CHO cells; ranges from 324-420
ChEMBL_27599 (CHEMBL644319) Displacement of [3H]DPCPX from human Adenosine A1 receptor expressed in CHO cells; ranges from 3420-3788
ChEMBL_27712 (CHEMBL639526) Displacement of [3H]-DPCPX from human Adenosine A1 receptor expressed in CHO cells; ranges from 2153-2891
ChEMBL_2931 (CHEMBL617646) In vitro ability to displace [3H]mesulergine binding from 5-hydroxytryptamine 2C receptor from bovine choroid plexus.
ChEMBL_2937 (CHEMBL617878) In vitro ability to displace [3H]mesulergine binding from 5-hydroxytryptamine 2C receptor from bovine choroid plexus.
ChEMBL_58484 (CHEMBL670415) Ability to displace [3H]spiperone from D2 dopamine receptor isolated from the striata of male Wistar rats
ChEMBL_58717 (CHEMBL671110) Compound was tested for the displacement of [3H]spiperone from Dopamine receptor D2 from rat striatal membranes.
ChEMBL_61408 (CHEMBL673349) Compound was tested for the displacement of [3H]spiperone from dopamine receptor D2 from rat striatal membranes.
ChEMBL_630234 (CHEMBL1105636) Displacement of [3H]deltorphin-2 from delta opioid receptor from Wistar rat brain by liquid scintillation counting
ChEMBL_63872 (CHEMBL671334) Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL_1343944 (CHEMBL3259253) Inhibition of HMG-coA reductase in CD rat liver microsomal-cytosol fraction assessed as inhibition of total lipid synthesis using [2-14C]acetate as substrate after 90 mins by scintillation counting analysis
ChEMBL_1343945 (CHEMBL3259254) Inhibition of HMG-coA reductase in CD rat liver microsomal-cytosol fraction assessed as inhibition of nonsaponifiable lipid synthesis using [2-14C]acetate as substrate after 90 mins by scintillation counting analysis
ChEMBL_1343946 (CHEMBL3259255) Inhibition of HMG-coA reductase in CD rat liver microsomal-cytosol fraction assessed as inhibition of fatty acid synthesis using [2-14C]acetate as substrate after 90 mins by scintillation counting analysis
ChEMBL_2018313 (CHEMBL4671891) Inhibition of FP-Rh binding to APT-1/2 in mouse brain cytosolic fraction preincubated for 1 hr followed by FP-Rh addition and measured after 1 hr by SDS-PAGE analysis
ChEMBL_808211 (CHEMBL1961123) Inhibition of 5-lipoxygenase in S100 cell free fraction of human polymorphonuclear leukocytes assessed as reduction in 5-LO product formation preincubated for 15 mins measured after 10 mins by HPLC analysis
ChEBML_139205 Displacement of [3H]pirenzepine from M1 receptor
ChEBML_144597 Inhibition of NEP 24.11 from rat kidney
ChEBML_153990 Tested for inhibition of pepsin from porcine
ChEBML_155205 Inhibition of phosphodiesterase 5 from human platelets
ChEBML_155368 Inhibition of Phosphodiesterase 5 from rat diaphragm
ChEBML_156630 Inhibition of Phosphodiesterase 3 from rabbit platelets
ChEBML_156890 Inhibition of PDE4 from guinea pig macrophages
ChEBML_195970 Tested for inhibition of renin from human
ChEBML_202161 Displacement of [3H]-citalopram from Serotonin transporter
ChEBML_213092 Inhibition of TXA2 synthetase from human platelets
ChEBML_225607 Inhibition of thymidylate synthase from L1210 cells
ChEBML_28302 Inhibition of Acetylcholinesterase (AChE) from human RBC
ChEBML_29235 Inhibition of acetylcholinesterase from rat striatal tissue
ChEBML_32354 Inhibitory activity towards Alpha-mannosidase from Almond
ChEBML_36274 Displacement of DHT from human androgen receptor
ChEBML_37428 Inhibitory activity towards Beta-Glucosidase from Almond
ChEBML_39370 Inhibition of beta-galactosidase from Aspergillus niger
ChEBML_48493 Inhibition of Cathepsin L from human kidney
ChEBML_49616 Tested for inhibition of Chymotrypsinogen from bovine
ChEBML_62807 Displacement of [3H]mazindol from dopamine transporter
ChEBML_67666 Displacement of radioligand from Estrogen receptor alpha
ChEBML_71399 Displacement of Dexamethasone from human glucocorticoid receptor
ChEMBL_1477140 (CHEMBL3428449) Displacement of MK499 from human ERG
ChEMBL_1542591 (CHEMBL3744630) Displacement of doferilide from human ERG
ChEMBL_155200 (CHEMBL763673) Inhibition of Phosphodiesterase 5 from human
ChEMBL_159885 (CHEMBL856203) Inhibition against Prolidase from pig kidney.
ChEMBL_1867235 (CHEMBL4368210) Inhibition of AChE from human erythrocytes
ChEMBL_2266263 Displacement of [3H]-dofetilide from human ERG
ChEMBL_2285335 Displacement of ssDNA from FTO (unknown origin)
ChEMBL_2324826 Displacement of [3H]Dofetilide from human ERG
ChEMBL_2475025 Displacement of [3H]-NF608 from rat GluK1
ChEMBL_2475026 Displacement of [3H]-KA from rat GluK2
ChEMBL_2475027 Displacement of [3H]-KA from rat GluK3
ChEMBL_326608 (CHEMBL863451) Displacement of [3H]citalopram from SERT
ChEMBL_326609 (CHEMBL863452) Displacement of [3H]nisoxetine from NET
ChEMBL_330473 (CHEMBL869979) Displacement of [3H]citalopram from SERT
ChEMBL_330474 (CHEMBL869980) Displacement of [3H]nisoxetine from NET
ChEMBL_335144 (CHEMBL867624) Displacement of [3H]nisoxetine from NET
ChEMBL_338547 (CHEMBL867191) Displacement of [3H]paroxetine from SERT
ChEMBL_355134 (CHEMBL853187) Displacement of [3H]citalopram from SERT
ChEMBL_355136 (CHEMBL853189) Displacement of [3H]nisoxetine from NET
ChEMBL_372848 (CHEMBL871130) Displacement of GM-BODIPY from Hsp90
ChEMBL_394938 (CHEMBL908048) Displacement of cy3B-GM from Hsp90alpha
ChEMBL_408752 (CHEMBL909940) Displacement of [3H]dofetilide from hERG
ChEMBL_41424 (CHEMBL654404) Inhibition of butyrylcholinesterase from human serum
ChEMBL_424080 (CHEMBL855083) Displacement of Fluormone from PPAR gamma
ChEMBL_428079 (CHEMBL914810) Displacement of [3H]PDBu from PKCalpha
ChEMBL_429832 (CHEMBL915413) Displacement of [3H]nisoxetine from NET
ChEMBL_429833 (CHEMBL915414) Displacement of [3H]paroxetine from 5HTT
ChEMBL_431029 (CHEMBL915899) Displacement of [3H]nisoxetine from NET
ChEMBL_431030 (CHEMBL915900) Displacement of [3H]paroxetine from 5HTT
ChEMBL_436364 (CHEMBL904672) Displacement of MIP1alpha from CCR5 receptor
ChEMBL_439699 (CHEMBL888810) Displacement of [3H]nisoxitine from NET
ChEMBL_439700 (CHEMBL888811) Displacement of [3H]citalopram from SERT
ChEMBL_447297 (CHEMBL896330) Displacement of [3H]haTRAP from PAR1
ChEMBL_457336 (CHEMBL940927) Displacement of [3H]bufuralol from CYP2D6
ChEMBL_486185 (CHEMBL1016593) Displacement of [3H]LTB4 from LTB4R
ChEMBL_492351 (CHEMBL948347) Displacement of [3H]nisoxetine from NET
ChEMBL_492352 (CHEMBL948348) Displacement of [3H]paroxetine from 5HTT
ChEMBL_512437 (CHEMBL980778) Displacement of radioligand from 5HT2B receptor
ChEMBL_512440 (CHEMBL980781) Displacement of radioligand from TXA2 receptor
ChEMBL_51851 (CHEMBL664074) Inhibition of cruzain from Trypanosoma cruzi
ChEMBL_537767 (CHEMBL989012) Displacement of [3H]paroxitine from SERT
ChEMBL_537768 (CHEMBL989013) Displacement of [3H]nisoxitine from NET
ChEMBL_556525 (CHEMBL956520) Inhibition of acetylcholinesterase from bovine erythrocyte
ChEMBL_560896 (CHEMBL1013531) Inhibition of BuChE from equine serum
ChEMBL_560915 (CHEMBL1013550) Displacement of [3H]paroxetine from 5HTT
ChEMBL_560916 (CHEMBL1013551) Displacement of [3H]nisoxetine from NET
ChEMBL_565897 (CHEMBL960843) Displacement of radioligand from EP1 receptor
ChEMBL_565898 (CHEMBL960018) Displacement of radioligand from EP2 receptor
ChEMBL_565899 (CHEMBL960019) Displacement of radioligand from EP4 receptor
ChEMBL_565900 (CHEMBL960020) Displacement of radioligand from IP receptor
ChEMBL_565901 (CHEMBL960021) Displacement of radioligand from FP receptor
ChEMBL_566227 (CHEMBL963308) Displacement of IL8 from CXCR1 receptor
ChEMBL_566228 (CHEMBL963309) Displacement of IL8 from CXCR2 receptor
ChEMBL_566867 (CHEMBL958367) Displacement of [3H]citalopram from SERT
ChEMBL_566868 (CHEMBL958368) Displacement of [3H]nisoxetine from NET
ChEMBL_570822 (CHEMBL789930) Displacement of [3H]glycine from GlyT2
ChEMBL_579372 (CHEMBL1063213) Displacement of radioligand from RARalpha receptor
ChEMBL_579373 (CHEMBL1063214) Displacement of radioligand from RARbeta receptor
ChEMBL_579374 (CHEMBL1063215) Displacement of radioligand from RARgamma receptor
ChEMBL_587779 (CHEMBL1040430) Displacement of [3H]nisoxetine from NET
ChEMBL_593412 (CHEMBL1040540) Displacement of dofetilide from human ERG
ChEMBL_625166 (CHEMBL1115187) Displacement of dofetilide from human ERG
ChEMBL_635391 (CHEMBL1120062) Displacement of labeled ITAC from CXCR3
ChEMBL_635407 (CHEMBL1120207) Displacement of labeled IP10 from CXCR3
ChEMBL_652722 (CHEMBL1225925) Displacement of radioligand from human GPR109A
ChEMBL_652723 (CHEMBL1225926) Displacement of radioligand from human GPR109B
ChEMBL_652725 (CHEMBL1225928) Displacement of radioligand from rat GPR109A
ChEMBL_69696 (CHEMBL682031) Inhibition of falcipain2 from Plasmodium falciparum
ChEMBL_70142 (CHEMBL685965) Inhibition of Farnesyltransferase from bovine brain
ChEMBL_70742 (CHEMBL681453) Inhibition of Farnesyltransferase from rat brain
ChEMBL_726913 (CHEMBL1686702) Displacement of radiolabeled Dexamethasone from GR
ChEMBL_727753 (CHEMBL1686112) Displacement of dofetilide from human ERG
ChEMBL_728108 (CHEMBL1687050) Displacement of radiolabeled Dexamethasone from GR
ChEMBL_792911 (CHEMBL1929757) Displacement of [3H]dexomethasone from GR
ChEMBL_792912 (CHEMBL1929758) Displacement of [3H]testosterone from AR
ChEMBL_792913 (CHEMBL1929759) Displacement of [3H]progesterone from PR
ChEMBL_797977 (CHEMBL1942854) Displacement of dofetilide from human ERG
ChEMBL_802791 (CHEMBL1953525) Displacement of dofetidine from human Erg
ChEMBL_811993 (CHEMBL2013363) Displacement of dofetilide from human ERG
ChEMBL_812135 (CHEMBL2013639) Displacement of dofetilide from human ERG
ChEMBL_812892 (CHEMBL2020267) Displacement of dofetilide from human ERG
ChEMBL_821302 (CHEMBL2040132) Displacement of dofetilide from human ERG
ChEMBL_833993 (CHEMBL2072733) Displacement of [3H]NAM from mGluR5
ChEMBL_878181 (CHEMBL2184102) Displacement of dofetilide from human ERG
ChEBML_146646 Ability to displace [3H]DPDPE from Opioid receptor delta 1 in rat brain membranes, was determined from radioreceptor assay.
ChEBML_148544 Ability to displace [3H]CTOP from Opioid receptor mu 1 in rat brain membranes, was determined from radioreceptor assay
ChEBML_47664 Compound was evaluated for its ability to displace [3H]-L-364,718 from Cholecystokinin type A receptor from rat pancreas
ChEBML_50042 Compound was evaluated for its ability to displace [3H]L-364718 from Cholecystokinin type A receptor from rat pancreas
ChEBML_90104 Compound was evaluated for its ability to displace [3H]Ins(1,4,5)P3 from membranes prepared from bovine adrenal corticles
ChEMBL_142637 (CHEMBL746905) Binding affinity for Norepinephrine transporter is assessed from the ability to displace [3H]nisoxetine from rat frontal cortex
ChEMBL_146553 (CHEMBL754971) The ability to displace [3H]naloxone from the opioid receptor mu isolated from rat brain membrane; >= no displacement
ChEMBL_2081762 (CHEMBL4737553) Displacement of [3H]quisqualate from mGluR1 from rat brain incubated for 60 mins by radiometric scintillation counting analysis
ChEMBL_2263961 Displacement of [3H]cyclohexyladen from A1 adenosine receptor derived from in guinea pig brain membrane assessed as inhibition constant
ChEMBL_2480417 Displacement of [3H]-LSD from human 5-HT6 receptor extracted from HEK293 cell membrane by microbeta plate reader analysis
ChEMBL_28020 (CHEMBL641219) In vitro inhibitory concentration against Muscarinic acetylcholine receptor derived from smooth muscle cells from thoracic aorta of monkeys
ChEMBL_31507 (CHEMBL647492) Displacement of [3H]-SCH- 58261 from human Adenosine A2A receptor expressed in HEK293 cells; ranges from 4.95-6.08
ChEMBL_833575 (CHEMBL2066516) Displacement of [125I] echistatin from alphaVbeta3 integrin isolated from human placenta after 3 hrs by liquid scintillation counter
Biochemical Assay Fluorescence polarization-based kinase in vitro assay using human PI3K alpha purchased from Echelon Biosciences and p110 alpha/p85 alpha from Upstate follow by a Kinase Glo assay from Promega.
HDAC Enzyme Activity Assay For the enzyme assay, the enzyme fraction was added to fluorescent substrate in the presence of test compounds, and the mixture was incubated for additional 30 min. The released aminomethyl coumarin (AMC) was measured using a fluorescence plate reader. The 50% inhibitory concentrations (IC50) were determined as means with SD calculated from at least three independent dose response curves.
Inhibition Assay An MGAT2 inhibition test for test compounds was conducted in accordance with a partially modified version of the method described in John F. Lockwood et al., Am. J. Physiol. Endocrinol. Metab., 2003, 285, E927.A 10 mg/mL microsomal fraction of human small intestine (duodenum- and jejunum-derived fraction purchased from Becton Dickinson Japan) was used as an enzyme source.The test was conducted using a flat-bottom 96-well plate (Corning).A buffer solution with final concentrations of 5 mM magnesium chloride, 1.25 mg/ml bovine serum albumin and 100 mM Tris-HCl (pH=7.5) was prepared and the microsomal fraction of human small intestine was added thereto to give a final concentration of 5 .mu.g/ml. Test compounds prepared in various concentrations using dimethyl sulfoxide were added thereto to give a final dimethyl sulfoxide concentration of 1% and a reaction was performed at room temperature for 5 min.
ChEBML_144290 Inhibitory concentration required for the displacement of [3H]NT from neurotensin receptor in mouse; value ranges from 4-6 uM
ChEBML_162037 Inhibition of Purine nucleoside Phosphorylase from calf spleen at 1 mM PO4 determined by measuring 3H release from [3H]-inosine
ChEMBL_149149 (CHEMBL759240) The ability to displace [3H]naloxone from the Opioid receptor mu 1 isolated from rat brain membrane; >= no displacement
ChEMBL_1764025 (CHEMBL4199272) Displacement of [3H]-5-CT from from 5-HT7 receptor in rat hypothalamus membranes by Cheng-Prusoff equation analysis
ChEMBL_1910 (CHEMBL616965) Compound was tested for the displacement of [3H]ketanserin from serotonin 5-hydroxytryptamine 2 receptor from rat cortical membranes.
ChEMBL_2480419 Displacement of [3H]-ketanserin from human 5-HT2A receptor extracted from CHO-K1 cell membrane by microbeta plate reader analysis
ChEMBL_2480420 Displacement of [3H]-5-CT from human 5-HT7 receptor extracted from HEK293 cell membrane by microbeta plate reader analysis
ChEMBL_2486251 Displacement of [125I]MCH from human MCHR1 extracted from HEK293 cell membrane assessed as inhibition constant by competitive binding assay
ChEMBL_2486252 Displacement of [125I]MCH from rat MCHR1 extracted from HEK293 cell membrane assessed as inhibition constant by competitive binding assay
ChEMBL_28019 (CHEMBL641218) In vitro inhibitory concentration against Acyl coenzyme A:cholesterol acyltransferase derived from smooth muscle cells from thoracic aorta of monkeys
ChEMBL_28021 (CHEMBL641220) In vitro inhibitory concentration against acyl coenzyme A:cholesterol acyltransferase derived from smooth muscle cells from thoracic aorta of monkeys
ChEMBL_28501 (CHEMBL645930) In vitro inhibitory concentration against Acyl coenzyme A:cholesterol acyltransferase derived from smooth muscle cells from thoracic aorta of monkeys
ChEMBL_610840 (CHEMBL1064995) Displacement of [125I-N-Methyl-4-(4-bromoanilino)phthalimide from beta-amyloid plaques isolated from Alzheimer's disease patient brain
ChEMBL_638890 (CHEMBL1167598) Displacement of [3H](+)-pentazocine from sigma1 opioid receptor from guinea pig brain cortex after 150 mins by scintillation counting
ChEMBL_70316 (CHEMBL678021) Equilibrium dissociation constant was measured from displacement of L-762,745 from Fibrinogen receptor of human platelets by flow cytometry
ChEBML_1716382 Inhibition of human full length NPP1 expressed in African green monkey COS7 cell membrane fraction using p-nitrophenyl-5'-thymidine monophosphate as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins
ChEBML_1716383 Inhibition of human full length NPP3 expressed in African green monkey COS7 cell membrane fraction using p-nitrophenyl-5'-thymidine monophosphate as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins
ChEBML_1716384 Inhibition of human NTPDase1 expressed in African green monkey COS7 cell membrane fraction using ATP as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by malachite green reagent-based assay
ChEBML_1716385 Inhibition of human NTPDase2 expressed in African green monkey COS7 cell membrane fraction using ATP as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by malachite green reagent-based assay
ChEBML_1716386 Inhibition of human NTPDase3 expressed in African green monkey COS7 cell membrane fraction using ATP as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by malachite green reagent-based assay
ChEBML_1716387 Inhibition of human NTPDase8 expressed in African green monkey COS7 cell membrane fraction using ATP as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by malachite green reagent-based assay
ChEBML_100077 Inhibition of Monoamine oxidase-B from Bovine liver
ChEBML_123499 Displacement of [3H]dexamethasone from human mineralocorticoid receptor
ChEBML_140490 Ability to displace [3H]glycine from NMDA receptor
ChEBML_159372 Displacement of [3H]dexamethasone from human progesterone receptor
ChEBML_1696080 Displacement of [3H]prazosin from human sigma1 receptor
ChEBML_1696081 Displacement of [3H]WAY100635 from human 5-HT1AR
ChEBML_305320 Inhibitory concentration against Beta Glucosidase from Caldocellum saccharolyticum
ChEBML_36109 Displacement of [3H]dexamethasone from human androgen receptor
ChEBML_36111 Displacement of [3H]mibolerone from human Androgen receptor
ChEBML_58603 Displacement of [3H]-spiperone from dopamine D2 receptor
ChEBML_62872 Displacement of [3H]spiperone from dopamine receptor D2
ChEBML_64504 50% Inhibitory potency against enkephalinase from mouse striatum.
ChEBML_67517 Displacement of [3H]estradiol from Estrogen receptor alpha
ChEBML_67826 Displacement of [3H]estradiol from Estrogen receptor beta
ChEBML_68665 Inhibition of Folyl-polyglutamate synthase from mouse liver
ChEBML_70046 potent inhibitor of GAR Tfase obtained from porcine
ChEMBL_144597 (CHEMBL747372) Inhibition of NEP 24.11 from rat kidney
ChEMBL_1506448 (CHEMBL3599847) Displacement of [3H]-Astemizole from human ERG
ChEMBL_1543914 (CHEMBL3749896) Displacement of dofetilide from human ERG channel
ChEMBL_155362 (CHEMBL762507) Inhibition of Phosphodiesterase 5 from porcine platelets
ChEMBL_155367 (CHEMBL762512) Inhibition of Phosphodiesterase 5 from rat diaphragm
ChEMBL_155368 (CHEMBL762513) Inhibition of Phosphodiesterase 5 from rat diaphragm
ChEMBL_155382 (CHEMBL760835) Inhibition of phosphodiesterase 6 from bovine retina
ChEMBL_155720 (CHEMBL760598) Inhibition of PDE4 enzyme from U937 cells
ChEMBL_155721 (CHEMBL760599) Inhibition of phosphodiesterase 4 from U937 cells
ChEMBL_155997 (CHEMBL764742) Inhibition of phosphodiesterase 1 from bovine heart
ChEMBL_156168 (CHEMBL760937) Inhibitory activity against PDE1 from cerebral cortex
ChEMBL_156628 (CHEMBL759873) Inhibition of phosphodiesterase 3 from rabbit platelets
ChEMBL_156629 (CHEMBL759874) Inhibition of phosphodiesterase 3 from rabbit platelets
ChEMBL_156636 (CHEMBL761134) Inhibitory activity against Phosphodiesterase 3 from heart.
ChEMBL_156890 (CHEMBL767080) Inhibition of PDE4 from guinea pig macrophages
ChEMBL_157048 (CHEMBL765691) Inhibition of PDE4 from U937 monocytic cells
ChEMBL_157364 (CHEMBL762040) Inhibition of Phosphodiesterase 4 from rat liver
ChEMBL_157397 (CHEMBL763662) Inhibitory activity against Phosphodiesterase 4 from heart.
ChEMBL_1680433 (CHEMBL4030710) Displacement of 3H-dofetilide from human ERG
ChEMBL_1793755 (CHEMBL4265674) Displacement of photoprobe from MPC2 (unknown origin)
ChEMBL_1855070 (CHEMBL4355799) Displacement of MK-0499 from human ERG
ChEMBL_1978282 (CHEMBL4611417) Displacement of [3H]astemizole from human ERG
ChEMBL_2132539 (CHEMBL4842054) Displacement of [125I]-CCL2 from mouse CCR2
ChEMBL_2271929 Displacement of [3H]CP55940 from human CB1 receptor
ChEMBL_2271930 Displacement of [3H]CP55940 from human CB2 receptor
ChEMBL_2285364 Displacement of [3H]-penicillin from Staphylococcus aureus PBP2a
ChEMBL_2285423 Displacement of [35S] GTPgammaS from human 5-HT1A
ChEMBL_304920 (CHEMBL827812) Inhibitory activity against alpha-Glucosidase from rice
ChEMBL_304922 (CHEMBL827814) Inhibitory activity against trehalase from porcine kidney
ChEMBL_304940 (CHEMBL826969) Inhibitory activity against alpha-Glucosidase from rice
ChEMBL_304941 (CHEMBL826970) Inhibitory activity against trehalase from porcine kidney
ChEMBL_305137 (CHEMBL832432) Inhibition of aldose reductase from pig lenses
ChEMBL_321236 (CHEMBL881771) Inhibitory activity against cathepsin B from human
ChEMBL_321237 (CHEMBL881772) Inhibitory activity against cathepsin L from human
ChEMBL_321238 (CHEMBL881773) Inhibitory activity against cathepsin S from human
ChEMBL_326653 (CHEMBL870558) Displacement of [3H]Citalopram from human SERT
ChEMBL_326654 (CHEMBL870559) Displacement of [3H]nisoxetine from human NET
ChEMBL_327776 (CHEMBL871142) Inhibitory activity against MurD from Escherichia coli
ChEMBL_327777 (CHEMBL863555) Inhibitory activity against MurD from Streptococcus pneumoniae
ChEMBL_331167 (CHEMBL854094) Displacement of [125I]DOI from human 5HT2A
ChEMBL_332366 (CHEMBL865196) Inhibitory activity against AChE from electric eel
ChEMBL_332367 (CHEMBL865200) Inhibitory activity against BuChE from horse serum
ChEMBL_335142 (CHEMBL867622) Displacement of [125I]RTI-55 from DAT
ChEMBL_335143 (CHEMBL867623) Displacement of [125I]RTI-55 from SERT
ChEMBL_366277 (CHEMBL867293) Displacement of [3H]nisoxetine from human NET
ChEMBL_366278 (CHEMBL867297) Displacement of [3H]paroxetine from human 5HTT
ChEMBL_37443 (CHEMBL648539) Inhibition of beta-glucosidase from Caldocellum saccharolyticum
ChEMBL_39370 (CHEMBL653245) Inhibition of beta-galactosidase from Aspergillus niger
ChEMBL_411464 (CHEMBL853861) Displacement of [125I]motilin from human MOTR
ChEMBL_431028 (CHEMBL915898) Displacement of [3H]WIN-35428 from DAT
ChEMBL_436135 (CHEMBL905537) Displacement of [3H]nisoxetine from rat NET
ChEMBL_437577 (CHEMBL906013) Displacement of radiolabeled Dexamethasone from human GR
ChEMBL_439670 (CHEMBL887619) Displacement of [3H]LSD from 5HT2B receptor
ChEMBL_439671 (CHEMBL887620) Displacement of [3H]mesulergine from 5HT2C receptor
ChEMBL_439784 (CHEMBL888894) Displacement of [3H]rosiglitazone from PPAR gamma
ChEMBL_453951 (CHEMBL885955) Displacement of [3H]MPEP from mGlu5 receptor
ChEMBL_454742 (CHEMBL886764) Displacement of [125I]hCG from LH receptor
ChEMBL_461812 (CHEMBL928941) Displacement of [125I]ITAC from CXCR3 receptor
ChEMBL_464828 (CHEMBL948223) Displacement of vitronectin from integrin alphavbeta3 receptor
ChEMBL_464829 (CHEMBL949296) Displacement of fibrinogen from integrin alpha2bbeta3 receptor
ChEMBL_464968 (CHEMBL947140) Inhibition of HDAC1 from human HeLa cells
ChEMBL_466360 (CHEMBL936370) Displacement of [125I]CCK8S from human CCK1R
ChEMBL_466361 (CHEMBL924691) Displacement of [125I]CCK8S from human CCK2R
ChEMBL_468124 (CHEMBL934144) Displacement of [3H]PGE2 from EP1 receptor
ChEMBL_479540 (CHEMBL931536) Displacement of radiolabeled Dexamethasone from glucocorticoid receptor
ChEMBL_486189 (CHEMBL1016597) Displacement of [3H]citalopram from serotonin transporter
ChEMBL_49497 (CHEMBL662792) Inhibition of bacterial collagenase from corynebacterium rathaii
ChEMBL_49607 (CHEMBL661258) Inhibitory activity against Chymotrypsinogen from Thermus flavus
ChEMBL_505994 (CHEMBL949646) Inhibition of aromatase from human placental microsomes
ChEMBL_514034 (CHEMBL976349) Displacement of radiolabeled dofetilide from human ERG
ChEMBL_514704 (CHEMBL976353) Displacement of [3H]cystisine from alpha4beta2 nAChR
ChEMBL_535414 (CHEMBL984443) Displacement of [3H]ketanserine from 5HT2A receptor
ChEMBL_537765 (CHEMBL994218) Displacement of [3H]mesulergine from 5HT2C receptor
ChEMBL_542151 (CHEMBL1009861) Displacement of [3H]ketanserin from 5HT2A receptor
ChEMBL_558174 (CHEMBL962308) Displacement of [3H]ketanserin from 5HT2A receptor
ChEMBL_563537 (CHEMBL961824) Displacement of [3H]SCH23390 from D1 receptor
ChEMBL_563771 (CHEMBL993534) Displacement of [3H]ketanserin from 5HT2A receptor
ChEMBL_563919 (CHEMBL965827) Displacement of radioligand from mu opioid receptor
ChEMBL_587777 (CHEMBL1040428) Displacement of [3H]WIN-35428 from DAT
ChEMBL_587778 (CHEMBL1040429) Displacement of [3H]paroxetine from 5-HTT
ChEMBL_599283 (CHEMBL1041011) Displacement of dofrtilide from human ERG channel
ChEMBL_604292 (CHEMBL1066748) Displacement of [3H]Citalopram from human SERT
ChEMBL_604293 (CHEMBL1066749) Displacement of [3H]Nisoxetine from human NET
ChEMBL_604294 (CHEMBL1066750) Displacement of [3H]DADLE from human DOR
ChEMBL_604295 (CHEMBL1066751) Displacement of [3H]U69593 from human KOR
ChEMBL_604296 (CHEMBL1066752) Displacement of [3H]DAMGO from human MOR
ChEMBL_624440 (CHEMBL1108768) Displacement of [3H]astemizole from human ERG
ChEMBL_625740 (CHEMBL1104417) Displacement of [3H]5CT from 5HT7 receptor
ChEMBL_626222 (CHEMBL1107989) Displacement of radiolabeled IL8 from CXCR2 receptor
ChEMBL_626224 (CHEMBL1107991) Displacement of radiolabeled MIP1beta from CCR5 receptor
ChEMBL_626225 (CHEMBL1107992) Displacement of radiolabeled IL8 from CXCR1 receptor
ChEMBL_626226 (CHEMBL1107993) Displacement of radiolabeled TARC from CCR4 receptor
ChEMBL_626227 (CHEMBL1107994) Displacement of radiolabeled MCP1 from CCR2b receptor
ChEMBL_626228 (CHEMBL1107995) Displacement of radiolabeled MIP1alpha from CCR1 receptor
ChEMBL_634136 (CHEMBL1119143) Displacement of [3H]paroxetine from 5HTT receptor
ChEMBL_634882 (CHEMBL1120514) Displacement of [3H]dofetilide from human ERG
ChEMBL_640796 (CHEMBL1175788) Displacement of radiolabeled astemizole from human ERG
ChEMBL_664671 (CHEMBL1260557) Displacement of [3H]dofetilide from human ERG
ChEMBL_675694 (CHEMBL1274055) Displacement of [3H]dofetilide from human ERG
ChEMBL_675705 (CHEMBL1272339) Displacement of radioligand from human EP1 receptor
ChEMBL_687332 (CHEMBL1292008) Displacement of [3H]-dofetilide from human ERG
ChEMBL_687415 (CHEMBL1292091) Displacement of [3H]-MPEP from human mGluR5
ChEMBL_698209 (CHEMBL1646514) Displacement of radioligand from mu opioid receptor
ChEMBL_698210 (CHEMBL1646515) Displacement of radioligand from kappa opioid receptor
ChEMBL_69925 (CHEMBL678805) Inhibition of GAR transformylase from Lactobacillus casei
ChEMBL_700343 (CHEMBL1647669) Displacement of [3H]dofetilide from human ERG
ChEMBL_70047 (CHEMBL681447) Inhibition of GAR transformylase from mammalian Manca
ChEMBL_716659 (CHEMBL1670484) Displacement of [3H]-dofetilide from human ERG
ChEMBL_744267 (CHEMBL1772074) Displacement of [3H]-MPEP from rat mGluR5
ChEMBL_784920 (CHEMBL1920312) Displacement of [3H]astemizole from human ERG
ChEMBL_795449 (CHEMBL1937454) Displacement of [125I]GIP from human GIPR
ChEMBL_795795 (CHEMBL1936682) Displacement of [3H]histamine from rat H1R
ChEMBL_795796 (CHEMBL1936683) Displacement of [3H]histamine from rat H3R
ChEMBL_795797 (CHEMBL1936684) Displacement of [3H]histamine from rat H4R
ChEMBL_795798 (CHEMBL1936685) Displacement of [3H]histamine from mouse H1R
ChEMBL_795799 (CHEMBL1936686) Displacement of [3H]histamine from mouse H3R
ChEMBL_796037 (CHEMBL1936570) Displacement of [3H]histamine from mouse H4R
ChEMBL_796233 (CHEMBL1938198) Displacement of [3H]dofetolide from human Erg
ChEMBL_800171 (CHEMBL1947733) Displacement of [125I]MIP-1beta from CCR5
ChEMBL_801017 (CHEMBL1948791) Displacement of [3H]dofetilide from human ERG
ChEMBL_815206 (CHEMBL2025223) Displacement of [3H]-17beta-estradiol from ERalpha
ChEMBL_815207 (CHEMBL2025224) Displacement of [3H]-17beta-estradiol from ERbeta
ChEMBL_819957 (CHEMBL2032544) Displacement of [3H]dofetilide from human ERG
ChEMBL_822867 (CHEMBL2037899) Displacement of [3H]dofetilide from human ERG
ChEMBL_834029 (CHEMBL2072769) Displacement of [125I]RTI-55 from DAT
ChEMBL_834030 (CHEMBL2072770) Displacement of [125I]ghrelin from GHS receptor
ChEMBL_834035 (CHEMBL2072775) Displacement of [3H]SR141716A from CB1 receptor
ChEMBL_848013 (CHEMBL2150564) Displacement of [3H]dofetilide from human ERG
ChEMBL_849882 (CHEMBL2148626) Displacement of [35S]MK499 from human ERG
ChEMBL_856088 (CHEMBL2162322) Displacement of [3H]-dofetilide from human ERG
ChEMBL_856840 (CHEMBL2163105) Displacement of [3H]-astemizole from human ERG
ChEMBL_858734 (CHEMBL2167045) Displacement of [125I]-IABN from D2 receptor
ChEMBL_858736 (CHEMBL2167047) Displacement of [125I]-IABN from D3 receptor
ChEMBL_872681 (CHEMBL2184661) Displacement of [3H]methylcarbamylcholine from alpha4beta2 nAChR
ChEMBL_874179 (CHEMBL2187911) Displacement of thiazene red from tau aggregate