Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4202007

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

Binding
Inhibition of human recombinant ALDH1A1 assessed as reduction in of NAD(P)H formation incubated for 2 mins by spectrophotometry
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Aldehyde dehydrogenase 1A1 (CHEMBL3577)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Based Optimization of a Novel Class of Aldehyde Dehydrogenase 1A (ALDH1A) Subfamily-Selective Inhibitors as Potential Adjuncts to Ovarian Cancer Chemotherapy.
Huddle BC, Grimley E, Buchman CD, Chtcherbinine M, Debnath B, Mehta P, Yang K, Morgan CA, Li S, Felton J, Sun D, Mehta G, Neamati N, Buckanovich RJ, Hurley TD, Larsen SD.
J Med Chem (2018) 61 : 8754 -8773
PubMed 30221940 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 6.31 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4210115 1 7.10
CHEMBL4213331 1 7.10
CHEMBL4214000 1 7.00
CHEMBL4205957 1 6.96
CHEMBL4205216 1 6.89
CHEMBL4216790 1 6.89
CHEMBL4204754 1 6.75
CHEMBL4209599 1 6.70
CHEMBL4205844 1 6.60
CHEMBL4214509 1 6.60
CHEMBL4208443 1 6.58
CHEMBL4217452 1 6.57
CHEMBL4218404 1 6.47
CHEMBL4218270 1 6.38
CHEMBL4218920 1 6.36
CHEMBL4217294 1 6.35
CHEMBL4205099 1 6.25
CHEMBL4204451 1 6.18
CHEMBL4206667 1 6.17
CHEMBL4217738 1 6.05
CHEMBL4209261 1 6.05
CHEMBL4210829 1 6.01
CHEMBL4213859 1 5.85
CHEMBL4211127 1 5.62
CHEMBL4213798 1 5.42
CHEMBL4218792 1 5.39
CHEMBL4210318 1 5.39
CHEMBL4213258 1 5.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4210115 IC50 = 80.0 nM 7.10
CHEMBL4213331 IC50 = 80.0 nM 7.10
CHEMBL4214000 IC50 = 100.0 nM 7.00
CHEMBL4205957 IC50 = 110.0 nM 6.96
CHEMBL4205216 IC50 = 130.0 nM 6.89
CHEMBL4216790 IC50 = 130.0 nM 6.89
CHEMBL4204754 IC50 = 180.0 nM 6.75
CHEMBL4209599 IC50 = 200.0 nM 6.70
CHEMBL4205844 IC50 = 250.0 nM 6.60
CHEMBL4214509 IC50 = 250.0 nM 6.60
CHEMBL4208443 IC50 = 260.0 nM 6.58
CHEMBL4217452 IC50 = 270.0 nM 6.57
CHEMBL4218404 IC50 = 340.0 nM 6.47
CHEMBL4218270 IC50 = 420.0 nM 6.38
CHEMBL4218920 IC50 = 440.0 nM 6.36
CHEMBL4217294 IC50 = 450.0 nM 6.35
CHEMBL4205099 IC50 = 560.0 nM 6.25
CHEMBL4204451 IC50 = 660.0 nM 6.18
CHEMBL4206667 IC50 = 670.0 nM 6.17
CHEMBL4217738 IC50 = 900.0 nM 6.05
CHEMBL4209261 IC50 = 890.0 nM 6.05
CHEMBL4210829 IC50 = 970.0 nM 6.01
CHEMBL4213859 IC50 = 1400.0 nM 5.85
CHEMBL4211127 IC50 = 2400.0 nM 5.62
CHEMBL4213798 IC50 = 3830.0 nM 5.42
CHEMBL4218792 IC50 = 4100.0 nM 5.39
CHEMBL4210318 IC50 = 4100.0 nM 5.39
CHEMBL4213258 IC50 = 8200.0 nM 5.09