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Assay Detail

CHEMBL4622628

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

Binding
Inhibition of recombinant AKR1C1 (unknown origin) assessed as reduction in S-tetralol-induced dehydrogenase activity by measuring NADPH level
7
Total Activities
7
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

Aldo-keto reductase family 1 member C1 (CHEMBL5905)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of Novel AKR1C3 Inhibitors as New Potential Treatment for Castration-Resistant Prostate Cancer.
Endo S, Oguri H, Segawa J, Kawai M, Hu D, Xia S, Okada T, Irie K, Fujii S, Gouda H, Iguchi K, Matsukawa T, Fujimoto N, Nakayama T, Toyooka N, Matsunaga T, Ikari A.
J Med Chem (2020) 63 : 10396 -10411
PubMed 32847363 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.22 5.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4644092 1 5.22
CHEMBL4640154 1 -
CHEMBL4646593 1 -
CHEMBL4648793 1 -
CHEMBL4639417 1 -
CHEMBL4640248 1 -
CHEMBL4634960 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4644092 IC50 = 6000.0 nM 5.22
CHEMBL4640154 IC50 > 10000.0 nM -
CHEMBL4646593 IC50 > 10000.0 nM -
CHEMBL4648793 IC50 > 10000.0 nM -
CHEMBL4639417 IC50 > 10000.0 nM -
CHEMBL4640248 IC50 > 10000.0 nM -
CHEMBL4634960 IC50 > 10000.0 nM -