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Assay Detail

CHEMBL3412867

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

Binding
Inhibition of Wistar rat lenses ALR2 using D,L-glyceraldehyde as substrate preincubated for 10 mins before substrate addition measured after 5 mins by spectrophotometry
38
Total Activities
38
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

Design and synthesis of potent and multifunctional aldose reductase inhibitors based on quinoxalinones.
Qin X, Hao X, Han H, Zhu S, Yang Y, Wu B, Hussain S, Parveen S, Jing C, Ma B, Zhu C.
J Med Chem (2015) 58 : 1254 -1267
PubMed 25602762 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 6.41 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3409347 1 7.50
CHEMBL3409362 1 7.25
CHEMBL3409344 1 7.20
CHEMBL3409348 1 7.16
CHEMBL56337 EPALRESTAT 4.0 1 7.08
CHEMBL3409349 1 7.04
CHEMBL3409345 1 7.02
CHEMBL3409346 1 6.86
CHEMBL3261531 1 6.84
CHEMBL3409367 1 6.82
CHEMBL3409363 1 6.80
CHEMBL3409366 1 6.74
CHEMBL3409357 1 6.72
CHEMBL3409353 1 6.62
CHEMBL3409361 1 6.56
CHEMBL3409356 1 6.53
CHEMBL3409360 1 6.50
CHEMBL3409358 1 6.49
CHEMBL3409352 1 6.43
CHEMBL3409343 1 6.40
CHEMBL3409364 1 6.40
CHEMBL3409355 1 6.38
CHEMBL3409369 1 6.38
CHEMBL3409359 1 6.33
CHEMBL3409354 1 6.33
CHEMBL3409351 1 6.19
CHEMBL3409371 1 6.19
CHEMBL3409370 1 6.10
CHEMBL3261527 1 6.09
CHEMBL3409339 1 6.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3409347 IC50 = 32.0 nM 7.50
CHEMBL3409362 IC50 = 56.0 nM 7.25
CHEMBL3409344 IC50 = 63.0 nM 7.20
CHEMBL3409348 IC50 = 69.0 nM 7.16
CHEMBL56337 EPALRESTAT IC50 = 84.0 nM 7.08
CHEMBL3409349 IC50 = 91.0 nM 7.04
CHEMBL3409345 IC50 = 95.0 nM 7.02
CHEMBL3409346 IC50 = 139.0 nM 6.86
CHEMBL3261531 IC50 = 143.0 nM 6.84
CHEMBL3409367 IC50 = 153.0 nM 6.82
CHEMBL3409363 IC50 = 158.0 nM 6.80
CHEMBL3409366 IC50 = 182.0 nM 6.74
CHEMBL3409357 IC50 = 191.0 nM 6.72
CHEMBL3409353 IC50 = 238.0 nM 6.62
CHEMBL3409361 IC50 = 273.0 nM 6.56
CHEMBL3409356 IC50 = 296.0 nM 6.53
CHEMBL3409360 IC50 = 319.0 nM 6.50
CHEMBL3409358 IC50 = 326.0 nM 6.49
CHEMBL3409352 IC50 = 368.0 nM 6.43
CHEMBL3409343 IC50 = 397.0 nM 6.40
CHEMBL3409364 IC50 = 395.0 nM 6.40
CHEMBL3409355 IC50 = 421.0 nM 6.38
CHEMBL3409369 IC50 = 419.0 nM 6.38
CHEMBL3409359 IC50 = 467.0 nM 6.33
CHEMBL3409354 IC50 = 468.0 nM 6.33
CHEMBL3409351 IC50 = 639.0 nM 6.19
CHEMBL3409371 IC50 = 652.0 nM 6.19
CHEMBL3409370 IC50 = 798.0 nM 6.10
CHEMBL3261527 IC50 = 820.0 nM 6.09
CHEMBL3409339 IC50 = 874.0 nM 6.06
CHEMBL3409365 IC50 = 1112.0 nM 5.95
CHEMBL3409340 IC50 = 1516.0 nM 5.82
CHEMBL3409341 IC50 = 2131.0 nM 5.67
CHEMBL3409342 IC50 = 2592.0 nM 5.59
CHEMBL3409350 IC50 = 3340.0 nM 5.48
CHEMBL3409338 IC50 = 3380.0 nM 5.47
CHEMBL3409368 IC50 = 4181.0 nM 5.38
CHEMBL1580909 IC50 = 5981.0 nM 5.22