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Assay Detail

CHEMBL4620143

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

Binding
Inhibition of AKR1B1 in rat lenses
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Aldo-keto reductase family 1 member B1 (CHEMBL2622)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Novel quinolin-4(1H)-one derivatives as multi-effective aldose reductase inhibitors for treatment of diabetic complications: Synthesis, biological evaluation, and molecular modeling studies.
Han Z, Zhu J, Zhang Y, Zhang Y, Zhang H, Qi G, Zhu C, Hao X.
Bioorg Med Chem Lett (2020) 30 : 127101 -127101
PubMed 32192796 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 5.93 7.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4644582 1 7.24
CHEMBL4634561 1 7.19
CHEMBL56337 EPALRESTAT 4.0 1 7.09
CHEMBL4641309 1 7.01
CHEMBL4637167 1 6.97
CHEMBL4635967 1 6.95
CHEMBL4648347 1 6.81
CHEMBL4636966 1 6.62
CHEMBL4648062 1 6.60
CHEMBL4640803 1 6.54
CHEMBL4647603 1 6.49
CHEMBL4639244 1 6.20
CHEMBL4633200 1 6.16
CHEMBL4641528 1 5.82
CHEMBL4640269 1 5.60
CHEMBL4639059 1 5.00
CHEMBL4637287 1 4.97
CHEMBL595369 1 4.96
CHEMBL608112 1 4.92
CHEMBL4647238 1 4.90
CHEMBL4644132 1 4.90
CHEMBL4648778 1 4.89
CHEMBL4646322 1 4.87
CHEMBL4638403 1 4.82
CHEMBL4643288 1 4.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4644582 IC50 = 57.0 nM 7.24
CHEMBL4634561 IC50 = 65.0 nM 7.19
CHEMBL56337 EPALRESTAT IC50 = 81.0 nM 7.09
CHEMBL4641309 IC50 = 98.0 nM 7.01
CHEMBL4637167 IC50 = 107.0 nM 6.97
CHEMBL4635967 IC50 = 112.0 nM 6.95
CHEMBL4648347 IC50 = 154.0 nM 6.81
CHEMBL4636966 IC50 = 237.0 nM 6.62
CHEMBL4648062 IC50 = 251.0 nM 6.60
CHEMBL4640803 IC50 = 287.0 nM 6.54
CHEMBL4647603 IC50 = 321.0 nM 6.49
CHEMBL4639244 IC50 = 626.0 nM 6.20
CHEMBL4633200 IC50 = 689.0 nM 6.16
CHEMBL4641528 IC50 = 1528.0 nM 5.82
CHEMBL4640269 IC50 = 2487.0 nM 5.60
CHEMBL4639059 IC50 = 9875.0 nM 5.00
CHEMBL4637287 IC50 = 10587.0 nM 4.97
CHEMBL595369 IC50 = 11017.0 nM 4.96
CHEMBL608112 IC50 = 12031.0 nM 4.92
CHEMBL4647238 IC50 = 12515.0 nM 4.90
CHEMBL4644132 IC50 = 12578.0 nM 4.90
CHEMBL4648778 IC50 = 12781.0 nM 4.89
CHEMBL4646322 IC50 = 13578.0 nM 4.87
CHEMBL4638403 IC50 = 15034.0 nM 4.82
CHEMBL4643288 IC50 = 15614.0 nM 4.81