Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL2046256

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

Binding
Inhibition of recombinant AKR1C2 assessed as NADP+ dependent oxidation of S-tetralol by fluorescence assay
110
Total Activities
110
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Development of potent and selective inhibitors of aldo-keto reductase 1C3 (type 5 17β-hydroxysteroid dehydrogenase) based on N-phenyl-aminobenzoates and their structure-activity relationships.
Adeniji AO, Twenter BM, Byrns MC, Jin Y, Chen M, Winkler JD, Penning TM.
J Med Chem (2012) 55 : 2311 -2323
PubMed 22263837 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 110 5.36 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL22815 1 6.82
CHEMBL2043313 1 6.72
CHEMBL2043318 1 6.72
CHEMBL2043310 1 6.66
CHEMBL2043319 1 6.57
CHEMBL1574420 1 6.55
CHEMBL2043314 1 6.55
CHEMBL2043320 1 6.54
CHEMBL23588 FLUFENAMIC ACID 2.0 1 6.43
CHEMBL23479 1 6.42
CHEMBL2043302 1 6.40
CHEMBL2043303 1 6.39
CHEMBL23832 FENAMIC ACID 1.0 1 6.36
CHEMBL2041001 1 6.31
CHEMBL2043300 1 6.29
CHEMBL2043321 1 6.27
CHEMBL1596993 1 6.16
CHEMBL2040884 1 6.16
CHEMBL2043316 1 6.06
CHEMBL2043307 1 6.04
CHEMBL2043322 1 6.04
CHEMBL2041002 1 6.04
CHEMBL2040851 1 6.01
CHEMBL2043305 1 5.97
CHEMBL1328677 1 5.96
CHEMBL2043323 1 5.96
CHEMBL2043299 1 5.89
CHEMBL2040997 1 5.88
CHEMBL2043304 1 5.84
CHEMBL2043311 1 5.83

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL22815 IC50 = 150.0 nM 6.82
CHEMBL2043318 IC50 = 190.0 nM 6.72
CHEMBL2043313 IC50 = 190.0 nM 6.72
CHEMBL2043310 IC50 = 220.0 nM 6.66
CHEMBL2043319 IC50 = 270.0 nM 6.57
CHEMBL1574420 IC50 = 280.0 nM 6.55
CHEMBL2043314 IC50 = 280.0 nM 6.55
CHEMBL2043320 IC50 = 290.0 nM 6.54
CHEMBL23588 FLUFENAMIC ACID IC50 = 370.0 nM 6.43
CHEMBL23479 IC50 = 380.0 nM 6.42
CHEMBL2043302 IC50 = 400.0 nM 6.40
CHEMBL2043303 IC50 = 410.0 nM 6.39
CHEMBL23832 FENAMIC ACID IC50 = 440.0 nM 6.36
CHEMBL2041001 IC50 = 490.0 nM 6.31
CHEMBL2043300 IC50 = 510.0 nM 6.29
CHEMBL2043321 IC50 = 540.0 nM 6.27
CHEMBL1596993 IC50 = 700.0 nM 6.16
CHEMBL2040884 IC50 = 700.0 nM 6.16
CHEMBL2043316 IC50 = 870.0 nM 6.06
CHEMBL2041002 IC50 = 910.0 nM 6.04
CHEMBL2043322 IC50 = 910.0 nM 6.04
CHEMBL2043307 IC50 = 920.0 nM 6.04
CHEMBL2040851 IC50 = 980.0 nM 6.01
CHEMBL2043305 IC50 = 1070.0 nM 5.97
CHEMBL2043323 IC50 = 1110.0 nM 5.96
CHEMBL1328677 IC50 = 1110.0 nM 5.96
CHEMBL2043299 IC50 = 1280.0 nM 5.89
CHEMBL2040997 IC50 = 1330.0 nM 5.88
CHEMBL2043304 IC50 = 1460.0 nM 5.84
CHEMBL2043311 IC50 = 1490.0 nM 5.83
CHEMBL2043315 IC50 = 1470.0 nM 5.83
CHEMBL2043301 IC50 = 1550.0 nM 5.81
CHEMBL2041557 IC50 = 1780.0 nM 5.75
CHEMBL2040993 IC50 = 1880.0 nM 5.73
CHEMBL2040891 IC50 = 2070.0 nM 5.68
CHEMBL2041000 IC50 = 2230.0 nM 5.65
CHEMBL2043309 IC50 = 2360.0 nM 5.63
CHEMBL2043312 IC50 = 2400.0 nM 5.62
CHEMBL2040994 IC50 = 2550.0 nM 5.59
CHEMBL2040887 IC50 = 2670.0 nM 5.57
CHEMBL2040999 IC50 = 2730.0 nM 5.56
CHEMBL2040996 IC50 = 2840.0 nM 5.55
CHEMBL1682199 4-PHENYLAMINO BENZOIC ACID IC50 = 3000.0 nM 5.52
CHEMBL2040893 IC50 = 3170.0 nM 5.50
CHEMBL2040886 IC50 = 3240.0 nM 5.49
CHEMBL2043306 IC50 = 3260.0 nM 5.49
CHEMBL1682200 IC50 = 3380.0 nM 5.47
CHEMBL2043308 IC50 = 3400.0 nM 5.47
CHEMBL2040995 IC50 = 3580.0 nM 5.45
CHEMBL2040888 IC50 = 3810.0 nM 5.42