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Assay Detail

CHEMBL1634174

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

Binding
Inhibition of Wistar rat lenses ALR2 by spectrophotometry
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Lens of camera-type eye
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

Acetic acid derivatives of 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide as a novel class of potent aldose reductase inhibitors.
Chen X, Zhu C, Guo F, Qiu X, Yang Y, Zhang S, He M, Parveen S, Jing C, Li Y, Ma B.
J Med Chem (2010) 53 : 8330 -8344
PubMed 21062005 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.51 7.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL84446 FIDARESTAT 2.0 1 7.54
CHEMBL1632036 1 7.50
CHEMBL1632033 1 7.39
CHEMBL1632040 1 7.28
CHEMBL1632032 1 7.18
CHEMBL1632037 1 7.15
CHEMBL1632029 1 7.05
CHEMBL1632034 1 7.03
CHEMBL1632030 1 6.97
CHEMBL1632027 1 6.96
CHEMBL1632038 1 6.94
CHEMBL1632024 1 6.90
CHEMBL1632025 1 6.66
CHEMBL1632035 1 6.22
CHEMBL1632039 1 6.17
CHEMBL1632031 1 6.03
CHEMBL1632026 1 6.01
CHEMBL1632044 1 4.85
CHEMBL1632041 1 4.23
CHEMBL1632042 1 4.13
CHEMBL1632028 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL84446 FIDARESTAT IC50 = 29.0 nM 7.54
CHEMBL1632036 IC50 = 32.0 nM 7.50
CHEMBL1632033 IC50 = 41.0 nM 7.39
CHEMBL1632040 IC50 = 52.0 nM 7.28
CHEMBL1632032 IC50 = 66.0 nM 7.18
CHEMBL1632037 IC50 = 71.0 nM 7.15
CHEMBL1632029 IC50 = 90.0 nM 7.05
CHEMBL1632034 IC50 = 94.0 nM 7.03
CHEMBL1632030 IC50 = 108.0 nM 6.97
CHEMBL1632027 IC50 = 111.0 nM 6.96
CHEMBL1632038 IC50 = 116.0 nM 6.94
CHEMBL1632024 IC50 = 125.0 nM 6.90
CHEMBL1632025 IC50 = 219.0 nM 6.66
CHEMBL1632035 IC50 = 595.0 nM 6.22
CHEMBL1632039 IC50 = 674.0 nM 6.17
CHEMBL1632031 IC50 = 931.0 nM 6.03
CHEMBL1632026 IC50 = 975.0 nM 6.01
CHEMBL1632044 IC50 = 14000.0 nM 4.85
CHEMBL1632041 IC50 = 58400.0 nM 4.23
CHEMBL1632042 IC50 = 74500.0 nM 4.13
CHEMBL1632028 IC50 = 101500.0 nM -