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Assay Detail

CHEMBL1909130

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

Binding
DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid)
1742
Total Activities
871
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Platelet
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

DrugMatrix in vitro pharmacology data
Scott S. Auerbach, DrugMatrix¨ and ToxFX¨ Coordinator National Toxicology Program

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 871 6.32 8.35
Ki 871 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL75435 DEXKETOPROFEN 4.0 2 8.35
CHEMBL1077 BROMFENAC 4.0 2 8.07
CHEMBL139 DICLOFENAC 4.0 2 7.89
CHEMBL469 KETOROLAC 4.0 2 7.89
CHEMBL571 KETOPROFEN 4.0 2 7.85
CHEMBL6 INDOMETHACIN 4.0 2 7.82
CHEMBL563 FLURBIPROFEN 4.0 2 7.68
CHEMBL1020 TOLMETIN 4.0 2 7.39
CHEMBL1908355 TENIDAP 2.0 2 7.26
CHEMBL175 DEXIBUPROFEN 4.0 2 6.98
CHEMBL686 MEFENAMIC ACID 4.0 2 6.94
CHEMBL1297 FENOPROFEN 4.0 2 6.84
CHEMBL828 PHENOTHIAZINE 2.0 2 6.71
CHEMBL509 MECLOFENAMIC ACID 4.0 2 6.69
CHEMBL154 NAPROXEN 4.0 2 6.68
CHEMBL521 IBUPROFEN 4.0 2 6.67
CHEMBL1333512 N,N'-DIPHENYL-P-PHENYLENEDIAMINE 2 6.58
CHEMBL954 ENCLOMIPHENE 3.0 2 6.46
CHEMBL727 THIOGUANINE 4.0 2 6.22
CHEMBL165 RESVERATROL 3.0 2 6.20
CHEMBL291338 3,3',4',5-TETRACHLOROSALICYLANILIDE 4.0 2 6.18
CHEMBL18797 SULINDAC SULFIDE -1.0 2 6.16
CHEMBL118 CELECOXIB 4.0 2 6.14
CHEMBL319244 CAFFEIC ACID PHENETHYL ESTER 2 6.08
CHEMBL1071 OXAPROZIN 4.0 2 6.07
CHEMBL413965 FELBINAC 3.0 2 6.05
CHEMBL1388 MONOBENZONE 4.0 2 5.99
CHEMBL63323 NIFLUMIC ACID 2.0 2 5.97
CHEMBL302795 TENOXICAM 2.0 2 5.94
CHEMBL56367 NIMESULIDE 4.0 2 5.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL75435 DEXKETOPROFEN IC50 = 4.483 nM 8.35
CHEMBL1077 BROMFENAC IC50 = 8.481 nM 8.07
CHEMBL139 DICLOFENAC IC50 = 13.0 nM 7.89
CHEMBL469 KETOROLAC IC50 = 13.0 nM 7.89
CHEMBL571 KETOPROFEN IC50 = 14.0 nM 7.85
CHEMBL6 INDOMETHACIN IC50 = 15.0 nM 7.82
CHEMBL563 FLURBIPROFEN IC50 = 21.0 nM 7.68
CHEMBL1020 TOLMETIN IC50 = 41.0 nM 7.39
CHEMBL1908355 TENIDAP IC50 = 55.0 nM 7.26
CHEMBL175 DEXIBUPROFEN IC50 = 105.0 nM 6.98
CHEMBL686 MEFENAMIC ACID IC50 = 116.0 nM 6.94
CHEMBL1297 FENOPROFEN IC50 = 145.0 nM 6.84
CHEMBL828 PHENOTHIAZINE IC50 = 196.0 nM 6.71
CHEMBL509 MECLOFENAMIC ACID IC50 = 203.0 nM 6.69
CHEMBL154 NAPROXEN IC50 = 211.0 nM 6.68
CHEMBL521 IBUPROFEN IC50 = 212.0 nM 6.67
CHEMBL1333512 N,N'-DIPHENYL-P-PHENYLENEDIAMINE IC50 = 260.0 nM 6.58
CHEMBL954 ENCLOMIPHENE IC50 = 346.0 nM 6.46
CHEMBL727 THIOGUANINE IC50 = 601.0 nM 6.22
CHEMBL165 RESVERATROL IC50 = 625.0 nM 6.20
CHEMBL291338 3,3',4',5-TETRACHLOROSALICYLANILIDE IC50 = 666.0 nM 6.18
CHEMBL18797 SULINDAC SULFIDE IC50 = 688.0 nM 6.16
CHEMBL118 CELECOXIB IC50 = 723.0 nM 6.14
CHEMBL319244 CAFFEIC ACID PHENETHYL ESTER IC50 = 833.0 nM 6.08
CHEMBL1071 OXAPROZIN IC50 = 856.0 nM 6.07
CHEMBL413965 FELBINAC IC50 = 894.0 nM 6.05
CHEMBL1388 MONOBENZONE IC50 = 1019.0 nM 5.99
CHEMBL63323 NIFLUMIC ACID IC50 = 1064.0 nM 5.97
CHEMBL302795 TENOXICAM IC50 = 1140.0 nM 5.94
CHEMBL56367 NIMESULIDE IC50 = 1226.0 nM 5.91
CHEMBL527 PIROXICAM IC50 = 1313.0 nM 5.88
CHEMBL599 MELOXICAM IC50 = 1319.0 nM 5.88
CHEMBL294199 CAPSAICIN IC50 = 1551.0 nM 5.81
CHEMBL24944 TRIBROMSALAN IC50 = 2065.0 nM 5.68
CHEMBL622 ETODOLAC IC50 = 2649.0 nM 5.58
CHEMBL165790 IPRIFLAVONE IC50 = 2944.3 nM 5.53
CHEMBL1612004 IC50 = 3152.0 nM 5.50
CHEMBL526 PROPOFOL IC50 = 3832.0 nM 5.42
CHEMBL1105 6-METHOXY-2-NAPHTHYLACETIC ACID IC50 = 4113.0 nM 5.39
CHEMBL25 ASPIRIN IC50 = 4192.0 nM 5.38
CHEMBL83 TAMOXIFEN IC50 = 4391.0 nM 5.36
CHEMBL411 DIETHYLSTILBESTROL IC50 = 5600.0 nM 5.25
CHEMBL195437 4-OCTYLPHENOL IC50 = 10319.0 nM 4.99
CHEMBL1425 MERCAPTOPURINE ANHYDROUS IC50 = 16242.0 nM 4.79
CHEMBL122 ROFECOXIB IC50 = 31868.0 nM 4.50
CHEMBL45 MELATONIN IC50 - -
CHEMBL92401 IPRONIAZID IC50 - -
CHEMBL1618305 NALOXONAZINE Ki - -
CHEMBL1909068 Ki - -
CHEMBL1618305 NALOXONAZINE IC50 - -