Target (4)
Compound (24)
Article Title (9)
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Assay (19)
asparaginyl endopeptidase (ae) hiv-1 protease ae pretherapy isolated ae protease mutant (v82f) hiv-1 protease ae-p (v3i, l10i, i13v, l33i, e35d, m36i, s37n, r41k, i54v, l63h, h69k, v82f, l89m)
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ChEBML_30285 AE maximal score at Adenosine A2A receptor ChEBML_30634 AE maximal score at Adenosine A3 receptor ChEMBL_28232 (CHEMBL638599) AE maximal score at Adenosine A1 receptor ChEMBL_30285 (CHEMBL642080) AE maximal score at Adenosine A2A receptor ChEMBL_158146 (CHEMBL767951) Inhibition of PG synthetase activity obtained from bovine seminal vesicles ChEMBL_2272266 Inhibition of human PHGDH using 3-PG as substrate by fluorescence based analysis ChEMBL_177029 (CHEMBL872009) In vitro inhibition of PGE-2 (PG) production in rat blood; 3-30 ChEMBL_1770013 (CHEMBL4222125) Inhibition of recombinant human PGAM1 using 3-PG as substrate by fluorescence based assay ChEMBL_860059 (CHEMBL2167995) Inhibition of ADAMTS-1 using FAM (5-carbosyfluorescein)-AE*LQGRPISIAK substrate after 2 hrs ChEMBL_2272267 Inhibition of human PHGDH using 3-PG as substrate incubated for 60 mins by fluorescence based analysis ChEMBL_772898 (CHEMBL1838301) Displacement of [1,2,6,7-3H]PG from human PR-LBD after 24 hrs by liquid scintillation counting ChEMBL_195775 (CHEMBL801066) In vitro inhibition of purified Human kidney renin (250 pg/mL) incubated with angiotensinogen at pH 7.2 COX Inhibitor Screening Assay The COX enzyme activities were measured using the COX Inhibitor Screening Assay kit provided by Cayman (Cayman, Chemical Co., Ann Arbor, MI). The assay directly measures PGF2a produced by SnCl2 reduction of COX-derived PGH2. This assay is based on the competition between prostaglandins (PGs) and a PG-acetylcholinesterase conjugate (PG tracer) for a limited amount of PG antiserum. IC50 values were calculated from the concentration-inhibition response curve (duplicate determinations). ChEMBL_2272269 Inhibition of human PHGDH expressed in Escherichia coli BL21 using 3-PG as substrate incubated for 30 mins by fluorescence based analysis ChEMBL_2058834 (CHEMBL4713835) Inhibition of recombinant PGAM1 (unknown origin) using 3-PG as substrate incubated for 2 mins in presence of ADP by microplate reader assay ChEMBL_1440170 (CHEMBL3383169) Antagonist activity against FFA2 receptor in human whole blood assessed as inhibition of sodium acetate-induced CD11b[AE] expression by flow cytometry ChEMBL_2058833 (CHEMBL4713834) Inhibition of recombinant His-tagged PGAM1 (unknown origin) expressed in Escherichia coli BL21 using 3-PG as substrate in presence of ADP by Kinase-Glo max luminescent assay ChEMBL_1624952 (CHEMBL3867364) Displacement of [1,2,6,7-3H]-PG from recombinant human GST-tagged PR-LBD (657 to 933 residues) expressed in baculovirus infected insect cells measured after 24 hrs by liquid scintillation counting method ChEMBL_1849703 (CHEMBL4350244) Mixed type inhibition of PHGDH (unknown origin) using 3-PG as substrate incubated for 20 mins in presence of , PSAT1, PSPH and varying NAD+ by diaphorase and resazurin dye based fluorescence assay
PG-L BDBM85502
BDBM210922 US9273043, AE
BDBM229667 US9334269, AE
US9273043, AE BDBM60942
BDBM134499 US8846656, 19-AE
BDBM204971 US9249085, I(ae)
BDBM293054 US10106501, Example AE
US20230357139, Compound AE BDBM634013
US8846656, 21-AE BDBM134516
BDBM197166 2-Palmitoylmonoglycerol (2-PG)
BDBM466330 US10799494, Compound PG-203
US10799494, Compound PG-128 BDBM466335
BDBM381041 US9890185, Example 15(ae)
BDBM381108 US9890185, Example 38(ae)
BDBM660451 US20240092799, Compound XXIX-AE
US12325697, Compound AE-2 BDBM747340
BDBM35279 tripeptide-based inhibitor, 14v AE-3763
US10941115, Example 17(ae) 4-[[4-[[4-[[5-tert-butyl-3-(methanesulfonamido)-2-methoxy-phenyl]carbamoylamino]-1-naphthyl]oxy]-2-pyridyl]amino]-2,6-dimethoxy-N-(2-morpholinoethyl)benzamide US9751837, Example 17(ae) BDBM298425 US10125100, Example 17(ae) US10392346, Example 17(ae)
PG Thromboxane B2 CAS_54397-85-2 THROMBOXANE B2 BDBM82210
BDBM23751 1-hexadecanoyl-2-(10-pyrenyldecanoyl)-sn-glycero-3-phosphoglycerol 1-palmitoyl-2-(10-pyrenyldecanoyl)-sn-glycero-3-phosphorylcholine beta-pyC-10-PG
BDBM50121264 PG-917 8-(2-Acetylamino-hexanoylamino)-22-[3-(diaminomethaniminium)-propyl]-19-(1H-indol-3-ylmethyl)-25-naphthalen-2-ylmethyl-7,10,18,21,24,27-hexaoxo-6,11,17,20,23,26-hexaaza-spiro[4.22]heptacosane-16-carboxylic acid CID44366154
BDBM50121257 PG-946 6-(2-Acetylamino-hexanoylamino)-20-[3-(diaminomethaniminium)-propyl]-17-(1H-indol-3-ylmethyl)-23-naphthalen-2-ylmethyl-5,8,16,19,22,25-hexaoxo-4,9,15,18,21,24-hexaaza-spiro[2.22]pentacosane-14-carboxylic acid amide CID44366186
BDBM50121267 CID44366214 5-(2-Acetylamino-hexanoylamino)-19-[3-(diaminomethaniminium)-propyl]-16-(1H-indol-3-ylmethyl)-22-naphthalen-2-ylmethyl-4,7,15,18,21,24-hexaoxo-tetracosahydro-3a,8,14,17,20,23-hexaaza-cyclopentacyclotricosene-13-carboxylic acid amide PG-901
CID44366181 BDBM50121258 PG-914 9-(2-Acetylamino-hexanoylamino)-23-[3-(diaminomethaniminium)-propyl]-20-(1H-indol-3-ylmethyl)-26-naphthalen-2-ylmethyl-8,11,19,22,25,28-hexaoxo-7,12,18,21,24,27-hexaaza-spiro[5.22]octacosane-17-carboxylic acid amide