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Assay Detail

CHEMBL655565

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Binding
Inhibitory activity against human Prostaglandin G/H synthase 2
ChEMBL ↗
52
Total Activities
52
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 2 (CHEMBL230) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective cyclooxygenase-2 inhibitors: heteroaryl modified 1,2-diarylimidazoles are potent, orally active antiinflammatory agents.
Khanna IK, Yu Y, Huff RM, Weier RM, Xu X, Koszyk FJ, Collins PW, Cogburn JN, Isakson PC, Koboldt CM, Masferrer JL, Perkins WE, Seibert K, Veenhuizen AW, Yuan J, Yang DC, Zhang YY.
J Med Chem (2000) 43 : 3168 -3185
PubMed 10956225 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 52 5.90 7.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL110382 — — 1 7.58
CHEMBL321156 — — 1 7.16
CHEMBL46712 — — 1 7.10
CHEMBL109017 — — 1 6.96
CHEMBL42225 — — 1 6.89
CHEMBL42561 — — 1 6.75
CHEMBL296447 — — 1 6.55
CHEMBL108936 — — 1 6.54
CHEMBL106023 — — 1 6.47
CHEMBL110660 — — 1 6.39
CHEMBL110331 — — 1 6.38
CHEMBL320926 — — 1 6.37
CHEMBL108452 — — 1 6.36
CHEMBL108961 — — 1 6.36
CHEMBL421417 — — 1 6.33
CHEMBL320790 — — 1 6.33
CHEMBL105766 — — 1 6.29
CHEMBL109143 — — 1 6.28
CHEMBL321216 — — 1 6.28
CHEMBL110446 — — 1 6.20
CHEMBL327078 — — 1 6.14
CHEMBL44466 — — 1 6.10
CHEMBL326639 — — 1 6.03
CHEMBL320330 — — 1 6.02
CHEMBL110876 — — 1 5.96
CHEMBL323954 — — 1 5.96
CHEMBL108978 — — 1 5.92
CHEMBL106151 — — 1 5.92
CHEMBL321881 — — 1 5.89
CHEMBL107600 — — 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL110382 — IC50 = 26.0 nM 7.58
CHEMBL321156 — IC50 = 70.0 nM 7.16
CHEMBL46712 — IC50 = 80.0 nM 7.10
CHEMBL109017 — IC50 = 110.0 nM 6.96
CHEMBL42225 — IC50 = 130.0 nM 6.89
CHEMBL42561 — IC50 = 180.0 nM 6.75
CHEMBL296447 — IC50 = 280.0 nM 6.55
CHEMBL108936 — IC50 = 290.0 nM 6.54
CHEMBL106023 — IC50 = 340.0 nM 6.47
CHEMBL110660 — IC50 = 410.0 nM 6.39
CHEMBL110331 — IC50 = 420.0 nM 6.38
CHEMBL320926 — IC50 = 430.0 nM 6.37
CHEMBL108961 — IC50 = 440.0 nM 6.36
CHEMBL108452 — IC50 = 440.0 nM 6.36
CHEMBL320790 — IC50 = 470.0 nM 6.33
CHEMBL421417 — IC50 = 470.0 nM 6.33
CHEMBL105766 — IC50 = 510.0 nM 6.29
CHEMBL109143 — IC50 = 520.0 nM 6.28
CHEMBL321216 — IC50 = 530.0 nM 6.28
CHEMBL110446 — IC50 = 630.0 nM 6.20
CHEMBL327078 — IC50 = 730.0 nM 6.14
CHEMBL44466 — IC50 = 790.0 nM 6.10
CHEMBL326639 — IC50 = 940.0 nM 6.03
CHEMBL320330 — IC50 = 950.0 nM 6.02
CHEMBL323954 — IC50 = 1100.0 nM 5.96
CHEMBL110876 — IC50 = 1100.0 nM 5.96
CHEMBL108978 — IC50 = 1200.0 nM 5.92
CHEMBL106151 — IC50 = 1200.0 nM 5.92
CHEMBL321881 — IC50 = 1300.0 nM 5.89
CHEMBL107600 — IC50 = 1500.0 nM 5.82
CHEMBL321016 — IC50 = 1540.0 nM 5.81
CHEMBL106192 — IC50 = 1700.0 nM 5.77
CHEMBL325755 — IC50 = 1690.0 nM 5.77
CHEMBL322136 — IC50 = 1800.0 nM 5.75
CHEMBL325790 — IC50 = 1800.0 nM 5.75
CHEMBL321407 — IC50 = 1830.0 nM 5.74
CHEMBL110145 — IC50 = 2800.0 nM 5.55
CHEMBL320961 — IC50 = 2900.0 nM 5.54
CHEMBL419561 — IC50 = 4150.0 nM 5.38
CHEMBL323277 — IC50 = 5800.0 nM 5.24
CHEMBL110574 — IC50 = 9600.0 nM 5.02
CHEMBL322720 — IC50 = 20700.0 nM 4.68
CHEMBL320318 — IC50 = 24400.0 nM 4.61
CHEMBL320118 — IC50 = 37600.0 nM 4.42
CHEMBL326005 — IC50 = 51000.0 nM 4.29
CHEMBL321898 — IC50 = 51000.0 nM 4.29
CHEMBL320986 — IC50 = 54000.0 nM 4.27
CHEMBL110448 — IC50 = 79000.0 nM 4.10
CHEMBL110462 — IC50 = 934000.0 nM -
CHEMBL420479 — IC50 > 100000.0 nM -