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Assay Detail

CHEMBL768737

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Concentration required to inhibit human prostaglandin G/H synthase 1 (COX-1) by 50%
96
Total Activities
96
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Prostaglandin G/H synthase 1 (CHEMBL221)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

1,2-Diarylimidazoles as potent, cyclooxygenase-2 selective, and orally active antiinflammatory agents.
Khanna IK, Weier RM, Yu Y, Xu XD, Koszyk FJ, Collins PW, Koboldt CM, Veenhuizen AW, Perkins WE, Casler JJ, Masferrer JL, Zhang YY, Gregory SA, Seibert K, Isakson PC.
J Med Chem (1997) 40 : 1634 -1647
PubMed 9171873 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 96 5.02 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6 INDOMETHACIN 4.0 1 7.00
CHEMBL298476 1 6.24
CHEMBL296447 1 5.96
CHEMBL296078 1 5.81
CHEMBL45192 1 5.80
CHEMBL46623 1 5.72
CHEMBL45197 1 5.68
CHEMBL47147 1 5.56
CHEMBL264300 1 5.52
CHEMBL42398 1 5.50
CHEMBL42674 1 5.45
CHEMBL296662 1 5.42
CHEMBL46584 1 5.35
CHEMBL297108 1 5.34
CHEMBL42996 1 5.30
CHEMBL298313 1 5.24
CHEMBL298269 1 5.21
CHEMBL290945 1 5.11
CHEMBL294967 1 5.09
CHEMBL289561 1 5.07
CHEMBL296673 1 4.92
CHEMBL44977 1 4.77
CHEMBL296984 1 4.71
CHEMBL44926 1 4.65
CHEMBL44516 1 4.64
CHEMBL297799 1 4.62
CHEMBL42561 1 4.58
CHEMBL296571 1 4.53
CHEMBL43493 1 4.52
CHEMBL43317 1 4.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6 INDOMETHACIN IC50 = 100.0 nM 7.00
CHEMBL298476 IC50 = 570.0 nM 6.24
CHEMBL296447 IC50 = 1100.0 nM 5.96
CHEMBL296078 IC50 = 1560.0 nM 5.81
CHEMBL45192 IC50 = 1600.0 nM 5.80
CHEMBL46623 IC50 = 1900.0 nM 5.72
CHEMBL45197 IC50 = 2100.0 nM 5.68
CHEMBL47147 IC50 = 2740.0 nM 5.56
CHEMBL264300 IC50 = 3000.0 nM 5.52
CHEMBL42398 IC50 = 3200.0 nM 5.50
CHEMBL42674 IC50 = 3540.0 nM 5.45
CHEMBL296662 IC50 = 3800.0 nM 5.42
CHEMBL46584 IC50 = 4500.0 nM 5.35
CHEMBL297108 IC50 = 4600.0 nM 5.34
CHEMBL42996 IC50 = 5000.0 nM 5.30
CHEMBL298313 IC50 = 5800.0 nM 5.24
CHEMBL298269 IC50 = 6200.0 nM 5.21
CHEMBL290945 IC50 = 7840.0 nM 5.11
CHEMBL294967 IC50 = 8200.0 nM 5.09
CHEMBL289561 IC50 = 8600.0 nM 5.07
CHEMBL296673 IC50 = 12000.0 nM 4.92
CHEMBL44977 IC50 = 17100.0 nM 4.77
CHEMBL296984 IC50 = 19300.0 nM 4.71
CHEMBL44926 IC50 = 22300.0 nM 4.65
CHEMBL44516 IC50 = 23000.0 nM 4.64
CHEMBL297799 IC50 = 24100.0 nM 4.62
CHEMBL42561 IC50 = 26000.0 nM 4.58
CHEMBL296571 IC50 = 29800.0 nM 4.53
CHEMBL43493 IC50 = 30000.0 nM 4.52
CHEMBL43317 IC50 = 35000.0 nM 4.46
CHEMBL432112 IC50 = 36000.0 nM 4.44
CHEMBL44829 IC50 = 42200.0 nM 4.38
CHEMBL42651 IC50 = 49000.0 nM 4.31
CHEMBL43103 IC50 = 53500.0 nM 4.27
CHEMBL43640 IC50 = 67000.0 nM 4.17
CHEMBL43672 IC50 = 67700.0 nM 4.17
CHEMBL417170 IC50 = 82000.0 nM 4.09
CHEMBL46712 IC50 = 90000.0 nM 4.05
CHEMBL43331 IC50 = 91000.0 nM 4.04
CHEMBL44468 IC50 > 100000.0 nM -
CHEMBL414162 IC50 > 100000.0 nM -
CHEMBL295752 IC50 > 100000.0 nM -
CHEMBL42074 IC50 > 100000.0 nM -
CHEMBL45090 IC50 > 100000.0 nM -
CHEMBL42223 IC50 > 100000.0 nM -
CHEMBL42408 IC50 > 100000.0 nM -
CHEMBL42225 IC50 = 723000.0 nM -
CHEMBL42119 IC50 > 100000.0 nM -
CHEMBL295654 IC50 > 100000.0 nM -
CHEMBL298296 IC50 > 100000.0 nM -