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Assay Detail

CHEMBL924228

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Binding
Inhibition of aldose reductase
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Aldo-keto reductase family 1 member B1 (CHEMBL1900)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Validation of an automated procedure for the prediction of relative free energies of binding on a set of aldose reductase inhibitors.
Ferrari AM, Degliesposti G, Sgobba M, Rastelli G.
Bioorg Med Chem (2007) 15 : 7865 -7877
PubMed 17870536 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 6.97 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL240725 1 9.00
CHEMBL20740 1 8.51
CHEMBL363387 LIDORESTAT 2.0 1 8.30
CHEMBL241577 1 8.22
CHEMBL241367 1 8.15
CHEMBL399598 1 7.96
CHEMBL334830 RANIRESTAT 3.0 1 7.82
CHEMBL240722 1 7.60
CHEMBL240721 1 7.54
CHEMBL395347 1 7.52
CHEMBL240720 1 7.46
CHEMBL84446 FIDARESTAT 2.0 1 7.46
CHEMBL10413 ZENARESTAT 2.0 1 7.36
CHEMBL7679 PONALRESTAT 2.0 1 7.25
CHEMBL273910 MINALRESTAT 2.0 1 7.14
CHEMBL239440 1 7.06
CHEMBL240719 1 6.97
CHEMBL241777 1 6.82
CHEMBL241572 1 6.75
CHEMBL335776 1 6.72
CHEMBL241570 1 6.64
CHEMBL84060 (R,S)-FIDARESTAT 1 6.24
CHEMBL240871 1 5.96
CHEMBL266497 SORBINIL 3.0 1 5.70
CHEMBL240714 1 5.46
CHEMBL240293 1 5.36
CHEMBL14184 HEXANOATE 1 4.17
CHEMBL1044 PHENYLACETIC ACID -1.0 1 4.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL240725 IC50 = 1.0 nM 9.00
CHEMBL20740 IC50 = 3.1 nM 8.51
CHEMBL363387 LIDORESTAT IC50 = 5.0 nM 8.30
CHEMBL241577 IC50 = 6.0 nM 8.22
CHEMBL241367 IC50 = 7.0 nM 8.15
CHEMBL399598 IC50 = 11.0 nM 7.96
CHEMBL334830 RANIRESTAT IC50 = 15.0 nM 7.82
CHEMBL240722 IC50 = 25.0 nM 7.60
CHEMBL240721 IC50 = 29.0 nM 7.54
CHEMBL395347 IC50 = 30.0 nM 7.52
CHEMBL240720 IC50 = 35.0 nM 7.46
CHEMBL84446 FIDARESTAT IC50 = 35.0 nM 7.46
CHEMBL10413 ZENARESTAT IC50 = 44.0 nM 7.36
CHEMBL7679 PONALRESTAT IC50 = 56.5 nM 7.25
CHEMBL273910 MINALRESTAT IC50 = 73.0 nM 7.14
CHEMBL239440 IC50 = 87.0 nM 7.06
CHEMBL240719 IC50 = 108.0 nM 6.97
CHEMBL241777 IC50 = 150.0 nM 6.82
CHEMBL241572 IC50 = 176.0 nM 6.75
CHEMBL335776 IC50 = 190.0 nM 6.72
CHEMBL241570 IC50 = 230.0 nM 6.64
CHEMBL84060 (R,S)-FIDARESTAT IC50 = 570.0 nM 6.24
CHEMBL240871 IC50 = 1100.0 nM 5.96
CHEMBL266497 SORBINIL IC50 = 2000.0 nM 5.70
CHEMBL240714 IC50 = 3500.0 nM 5.46
CHEMBL240293 IC50 = 4400.0 nM 5.36
CHEMBL14184 HEXANOATE IC50 = 68200.0 nM 4.17
CHEMBL1044 PHENYLACETIC ACID IC50 = 96000.0 nM 4.02