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Assay Detail

CHEMBL5350501

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

Binding
Inhibition of human recombinant AKR1C2 transfected in Escherichia coli BL21 (DE3) pLysS competent cells using S-tetralol as substrate assessed as inhibition of NADP+ dependent substrate oxidation incubated for 10 mins by fluorescence microplate reader assay
ChEMBL ↗
68
Total Activities
68
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Aldo-keto reductase family 1 member C2 (CHEMBL5847) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of Biaryl-Containing Aldo-Keto Reductase 1C3 (AKR1C3) Inhibitors for Reversing AKR1C3-Mediated Drug Resistance in Cancer Treatment.
He S, Chu X, Wu Y, Jiang J, Fang P, Chen Y, Liu Y, Qiu Z, Xiao Y, Li Z, Pan D, Zhang Q, Xie H, Xing S, Feng F, Liu W, Guo Q, Zhao L, Yang P, Sun H.
J Med Chem (2023) 66 : 9537 -9560
PubMed 37409679 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 68 6.11 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL194686 — — 1 6.89
CHEMBL5436838 — — 1 6.80
CHEMBL5401700 — — 1 6.70
CHEMBL5398882 — — 1 6.64
CHEMBL5405863 — — 1 6.62
CHEMBL5426283 — — 1 6.62
CHEMBL5419252 — — 1 6.62
CHEMBL5422601 — — 1 6.55
CHEMBL193971 — — 1 6.54
CHEMBL5419326 — — 1 6.52
CHEMBL5406588 — — 1 6.51
CHEMBL5439918 — — 1 6.47
CHEMBL5414784 — — 1 6.46
CHEMBL5396002 — — 1 6.43
CHEMBL5410510 — — 1 6.41
CHEMBL5434084 — — 1 6.40
CHEMBL5425327 — — 1 6.40
CHEMBL5439018 — — 1 6.36
CHEMBL5413682 — — 1 6.35
CHEMBL5423363 — — 1 6.35
CHEMBL5408142 — — 1 6.35
CHEMBL5416628 — — 1 6.33
CHEMBL5412756 — — 1 6.30
CHEMBL5413689 — — 1 6.28
CHEMBL563 FLURBIPROFEN 4.0 1 6.26
CHEMBL5400783 — — 1 6.24
CHEMBL5421222 — — 1 6.21
CHEMBL5419024 — — 1 6.21
CHEMBL5393766 — — 1 6.19
CHEMBL5437831 — — 1 6.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL194686 — IC50 = 130.0 nM 6.89
CHEMBL5436838 — IC50 = 160.0 nM 6.80
CHEMBL5401700 — IC50 = 200.0 nM 6.70
CHEMBL5398882 — IC50 = 230.0 nM 6.64
CHEMBL5405863 — IC50 = 240.0 nM 6.62
CHEMBL5426283 — IC50 = 240.0 nM 6.62
CHEMBL5419252 — IC50 = 240.0 nM 6.62
CHEMBL5422601 — IC50 = 280.0 nM 6.55
CHEMBL193971 — IC50 = 290.0 nM 6.54
CHEMBL5419326 — IC50 = 300.0 nM 6.52
CHEMBL5406588 — IC50 = 310.0 nM 6.51
CHEMBL5439918 — IC50 = 340.0 nM 6.47
CHEMBL5414784 — IC50 = 350.0 nM 6.46
CHEMBL5396002 — IC50 = 370.0 nM 6.43
CHEMBL5410510 — IC50 = 390.0 nM 6.41
CHEMBL5434084 — IC50 = 400.0 nM 6.40
CHEMBL5425327 — IC50 = 400.0 nM 6.40
CHEMBL5439018 — IC50 = 440.0 nM 6.36
CHEMBL5413682 — IC50 = 450.0 nM 6.35
CHEMBL5423363 — IC50 = 450.0 nM 6.35
CHEMBL5408142 — IC50 = 450.0 nM 6.35
CHEMBL5416628 — IC50 = 470.0 nM 6.33
CHEMBL5412756 — IC50 = 500.0 nM 6.30
CHEMBL5413689 — IC50 = 530.0 nM 6.28
CHEMBL563 FLURBIPROFEN IC50 = 550.0 nM 6.26
CHEMBL5400783 — IC50 = 570.0 nM 6.24
CHEMBL5419024 — IC50 = 620.0 nM 6.21
CHEMBL5421222 — IC50 = 610.0 nM 6.21
CHEMBL5393766 — IC50 = 640.0 nM 6.19
CHEMBL5437831 — IC50 = 650.0 nM 6.19
CHEMBL5421708 — IC50 = 660.0 nM 6.18
CHEMBL5398259 — IC50 = 660.0 nM 6.18
CHEMBL5428274 — IC50 = 700.0 nM 6.16
CHEMBL5406928 — IC50 = 710.0 nM 6.15
CHEMBL5427233 — IC50 = 710.0 nM 6.15
CHEMBL5437603 — IC50 = 740.0 nM 6.13
CHEMBL5426142 — IC50 = 780.0 nM 6.11
CHEMBL5431359 — IC50 = 780.0 nM 6.11
CHEMBL5437329 — IC50 = 790.0 nM 6.10
CHEMBL5427069 — IC50 = 810.0 nM 6.09
CHEMBL5404373 — IC50 = 840.0 nM 6.08
CHEMBL5436664 — IC50 = 850.0 nM 6.07
CHEMBL5401215 — IC50 = 920.0 nM 6.04
CHEMBL5409615 — IC50 = 970.0 nM 6.01
CHEMBL5403144 — IC50 = 1010.0 nM 6.00
CHEMBL5431987 — IC50 = 1080.0 nM 5.97
CHEMBL196945 — IC50 = 1100.0 nM 5.96
CHEMBL5436866 — IC50 = 1130.0 nM 5.95
CHEMBL5397312 — IC50 = 1170.0 nM 5.93
CHEMBL5419770 — IC50 = 1210.0 nM 5.92