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Assay Detail

CHEMBL2046255

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

Binding
Inhibition of recombinant AKR1C3 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 C3 (CHEMBL4681)
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 6.27 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1682200 1 7.52
CHEMBL2041555 1 7.52
CHEMBL2043307 1 7.52
CHEMBL2043300 1 7.40
CHEMBL2043305 1 7.40
CHEMBL2041554 1 7.40
CHEMBL2041556 1 7.40
CHEMBL2041557 1 7.40
CHEMBL23588 FLUFENAMIC ACID 2.0 1 7.30
CHEMBL1682201 1 7.30
CHEMBL2043310 1 7.22
CHEMBL1682202 1 7.22
CHEMBL2043303 1 7.16
CHEMBL2043313 1 7.10
CHEMBL2040884 1 7.10
CHEMBL1596993 1 7.05
CHEMBL2043302 1 6.89
CHEMBL1682204 1 6.89
CHEMBL2043301 1 6.85
CHEMBL2040999 1 6.85
CHEMBL1682203 1 6.85
CHEMBL22815 1 6.82
CHEMBL2043321 1 6.82
CHEMBL2041154 1 6.82
CHEMBL1574420 1 6.80
CHEMBL2043314 1 6.80
CHEMBL2043320 1 6.66
CHEMBL23479 1 6.62
CHEMBL2043322 1 6.60
CHEMBL2041001 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2041555 IC50 = 30.0 nM 7.52
CHEMBL1682200 IC50 = 30.0 nM 7.52
CHEMBL2043307 IC50 = 30.0 nM 7.52
CHEMBL2043300 IC50 = 40.0 nM 7.40
CHEMBL2041554 IC50 = 40.0 nM 7.40
CHEMBL2041556 IC50 = 40.0 nM 7.40
CHEMBL2041557 IC50 = 40.0 nM 7.40
CHEMBL2043305 IC50 = 40.0 nM 7.40
CHEMBL23588 FLUFENAMIC ACID IC50 = 50.0 nM 7.30
CHEMBL1682201 IC50 = 50.0 nM 7.30
CHEMBL1682202 IC50 = 60.0 nM 7.22
CHEMBL2043310 IC50 = 60.0 nM 7.22
CHEMBL2043303 IC50 = 70.0 nM 7.16
CHEMBL2043313 IC50 = 80.0 nM 7.10
CHEMBL2040884 IC50 = 80.0 nM 7.10
CHEMBL1596993 IC50 = 90.0 nM 7.05
CHEMBL2043302 IC50 = 130.0 nM 6.89
CHEMBL1682204 IC50 = 130.0 nM 6.89
CHEMBL2043301 IC50 = 140.0 nM 6.85
CHEMBL1682203 IC50 = 140.0 nM 6.85
CHEMBL2040999 IC50 = 140.0 nM 6.85
CHEMBL2043321 IC50 = 150.0 nM 6.82
CHEMBL2041154 IC50 = 150.0 nM 6.82
CHEMBL22815 IC50 = 150.0 nM 6.82
CHEMBL2043314 IC50 = 160.0 nM 6.80
CHEMBL1574420 IC50 = 160.0 nM 6.80
CHEMBL2043320 IC50 = 220.0 nM 6.66
CHEMBL23479 IC50 = 240.0 nM 6.62
CHEMBL2043322 IC50 = 250.0 nM 6.60
CHEMBL2041001 IC50 = 250.0 nM 6.60
CHEMBL2041558 IC50 = 250.0 nM 6.60
CHEMBL2041006 IC50 = 260.0 nM 6.58
CHEMBL1682205 IC50 = 280.0 nM 6.55
CHEMBL2041004 IC50 = 280.0 nM 6.55
CHEMBL2041158 IC50 = 290.0 nM 6.54
CHEMBL2041153 IC50 = 320.0 nM 6.50
CHEMBL2041559 IC50 = 360.0 nM 6.44
CHEMBL2043304 IC50 = 360.0 nM 6.44
CHEMBL2041160 IC50 = 460.0 nM 6.34
CHEMBL2040998 IC50 = 470.0 nM 6.33
CHEMBL1682206 IC50 = 490.0 nM 6.31
CHEMBL2043318 IC50 = 500.0 nM 6.30
CHEMBL2043319 IC50 = 500.0 nM 6.30
CHEMBL2041562 IC50 = 500.0 nM 6.30
CHEMBL2041156 IC50 = 560.0 nM 6.25
CHEMBL2041159 IC50 = 560.0 nM 6.25
CHEMBL1328677 IC50 = 570.0 nM 6.24
CHEMBL2043315 IC50 = 570.0 nM 6.24
CHEMBL2041000 IC50 = 600.0 nM 6.22
CHEMBL2041002 IC50 = 610.0 nM 6.21