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Assay Detail

CHEMBL5732256

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

Binding
In Vitro COX Assay: COX activity was measured using a commercial kit (COX Inhibitor Screening Assay Kit Cayman Chemical N. 560131) which includes both ovine COX-1 and human recombinant COX-2 enzymes. Inhibitors were pre-incubated with either ovine COX-1 or human COX-2 in order to screen isozyme-specific inhibition. Differently than described in the kit protocol, the reaction was carried out in the presence of 5 μM arachidonic acid while for the blank sample (no activity) the two enzymes were inactivated for 40 minutes at 100° C. It was then measured the amount of PGF2α produced by reduction with SnCl2 of COX-derived PGH2, via enzyme immunoassay (EIA) using a PG-specific antibody and competing with a PG-acetylcholinesterase conjugate.Absorbance was measured at 412 nm with a Tecan Infinite M200 plate reader and data were processed according to manufacturer's instructions.
ChEMBL ↗
66
Total Activities
19
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

Multitarget FAAH and COX inhibitors and therapeutical uses thereof
(2017)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.45 11.00
kon 22 - -
k_off 22 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3775041 — — 12 11.00
CHEMBL3775104 — — 3 7.70
CHEMBL3774442 — — 3 7.52
CHEMBL563 FLURBIPROFEN 4.0 3 6.82
CHEMBL3774467 — — 3 6.82
CHEMBL3774439 — — 3 6.58
CHEMBL3775979 — — 3 6.43
CHEMBL3774586 — — 3 6.24
CHEMBL3774541 — — 3 6.22
CHEMBL3775610 — — 3 6.14
CHEMBL3774873 — — 3 6.00
CHEMBL3775280 — — 3 5.96
CHEMBL3775392 — — 3 5.89
CHEMBL3775770 — — 3 5.68
CHEMBL3774805 — — 3 5.43
CHEMBL3775699 — — 3 5.36
CHEMBL3775973 — — 3 5.20
CHEMBL3775462 — — 3 5.10
CHEMBL3774867 — — 3 5.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3775041 — IC50 = 0.01 nM 11.00
CHEMBL3775041 — IC50 = 12.0 nM 7.92
CHEMBL3775041 — IC50 = 12.0 nM 7.92
CHEMBL3775104 — IC50 = 20.0 nM 7.70
CHEMBL3774442 — IC50 = 30.0 nM 7.52
CHEMBL3774467 — IC50 = 150.0 nM 6.82
CHEMBL563 FLURBIPROFEN IC50 = 150.0 nM 6.82
CHEMBL3774439 — IC50 = 260.0 nM 6.58
CHEMBL3775979 — IC50 = 370.0 nM 6.43
CHEMBL3774586 — IC50 = 580.0 nM 6.24
CHEMBL3774541 — IC50 = 600.0 nM 6.22
CHEMBL3775610 — IC50 = 720.0 nM 6.14
CHEMBL3774873 — IC50 = 990.0 nM 6.00
CHEMBL3775280 — IC50 = 1100.0 nM 5.96
CHEMBL3775392 — IC50 = 1300.0 nM 5.89
CHEMBL3775770 — IC50 = 2100.0 nM 5.68
CHEMBL3774805 — IC50 = 3700.0 nM 5.43
CHEMBL3775699 — IC50 = 4400.0 nM 5.36
CHEMBL3775973 — IC50 = 6300.0 nM 5.20
CHEMBL3775462 — IC50 = 7900.0 nM 5.10
CHEMBL3774867 — IC50 = 8200.0 nM 5.09
CHEMBL3775041 — IC50 = 13000.0 nM 4.89
CHEMBL3775610 — kon = - — -
CHEMBL3775041 — kon = - — -
CHEMBL3775610 — k_off = - s-1 -
CHEMBL3774442 — k_off = - s-1 -
CHEMBL3775973 — kon = - — -
CHEMBL3775462 — kon = - — -
CHEMBL3775462 — k_off = - s-1 -
CHEMBL3775699 — kon = - — -
CHEMBL3775699 — k_off = - s-1 -
CHEMBL3774867 — kon = - — -
CHEMBL3774867 — k_off = - s-1 -
CHEMBL3774541 — kon = - — -
CHEMBL3774541 — k_off = - s-1 -
CHEMBL3774467 — kon = - — -
CHEMBL3775041 — k_off = - s-1 -
CHEMBL3775041 — kon = - — -
CHEMBL3775770 — k_off = - s-1 -
CHEMBL3775770 — kon = - — -
CHEMBL3774442 — kon = - — -
CHEMBL563 FLURBIPROFEN kon = - — -
CHEMBL3775280 — k_off = - s-1 -
CHEMBL3775280 — kon = - — -
CHEMBL563 FLURBIPROFEN k_off = - s-1 -
CHEMBL3775041 — kon = - — -
CHEMBL3774873 — k_off = - s-1 -
CHEMBL3774873 — kon = - — -
CHEMBL3775041 — k_off = - s-1 -
CHEMBL3775041 — k_off = - s-1 -