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Assay Detail

CHEMBL4821208

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Binding
Inhibition of ALDH1A1 (unknown origin)
17
Total Activities
17
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

Development of new disulfiram analogues as ALDH1a1-selective inhibitors.
Omran Z.
Bioorg Med Chem Lett (2021) 40 : 127958 -127958
PubMed 33744437 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.50 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL120563 THIRAM 2.0 1 7.70
CHEMBL121556 1 7.40
CHEMBL121516 BIS(PIPERIDINYLTHIOCARBONYL)DISULFIDE 1 7.30
CHEMBL964 DISULFIRAM 4.0 1 6.89
CHEMBL4869675 1 6.82
CHEMBL4861113 1 6.77
CHEMBL4854915 1 6.68
CHEMBL578805 1 6.57
CHEMBL4858425 1 5.59
CHEMBL4858703 1 5.54
CHEMBL4878814 1 5.53
CHEMBL333177 1 5.25
CHEMBL4871643 1 -
CHEMBL120082 BIS(DIBENZYLAMINETHIOCARBONYL)DISULFIDE 1 -
CHEMBL1256137 CYSTEAMINE HYDROCHLORIDE 4.0 1 -
CHEMBL1594935 CYSTAMINE DIHYDROCHLORIDE 1 -
CHEMBL507900 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL120563 THIRAM IC50 = 20.0 nM 7.70
CHEMBL121556 IC50 = 40.0 nM 7.40
CHEMBL121516 BIS(PIPERIDINYLTHIOCARBONYL)DISULFIDE IC50 = 50.0 nM 7.30
CHEMBL964 DISULFIRAM IC50 = 130.0 nM 6.89
CHEMBL4869675 IC50 = 150.0 nM 6.82
CHEMBL4861113 IC50 = 170.0 nM 6.77
CHEMBL4854915 IC50 = 210.0 nM 6.68
CHEMBL578805 IC50 = 270.0 nM 6.57
CHEMBL4858425 IC50 = 2540.0 nM 5.59
CHEMBL4858703 IC50 = 2850.0 nM 5.54
CHEMBL4878814 IC50 = 2950.0 nM 5.53
CHEMBL333177 IC50 = 5610.0 nM 5.25
CHEMBL4871643 IC50 > 100000.0 nM -
CHEMBL120082 BIS(DIBENZYLAMINETHIOCARBONYL)DISULFIDE IC50 > 100000.0 nM -
CHEMBL1256137 CYSTEAMINE HYDROCHLORIDE IC50 - -
CHEMBL1594935 CYSTAMINE DIHYDROCHLORIDE IC50 > 100000.0 nM -
CHEMBL507900 IC50 - -