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Assay Detail

CHEMBL4479403

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

Binding
Inhibition of CYP17 (unknown origin)
15
Total Activities
15
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

Steroid 17-alpha-hydroxylase/17,20 lyase (CHEMBL3522)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of Novel Steroidal Androgen Receptor Degrading Agents Inspired by Galeterone 3β-Imidazole Carbamate.
Purushottamachar P, Kwegyir-Afful AK, Martin MS, Ramamurthy VP, Ramalingam S, Njar VC.
ACS Med Chem Lett (2016) 7 : 708 -713
PubMed 27437082 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 5.90 7.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL254328 ABIRATERONE 3.0 1 7.32
CHEMBL2105738 GALETERONE 3.0 1 6.85
CHEMBL4591875 1 6.32
CHEMBL4552506 1 4.59
CHEMBL4521939 1 4.41
CHEMBL1082407 ENZALUTAMIDE 4.0 1 -
CHEMBL4541575 1 -
CHEMBL4581336 1 -
CHEMBL4593419 1 -
CHEMBL4532487 1 -
CHEMBL4520316 1 -
CHEMBL4539707 1 -
CHEMBL4588643 1 -
CHEMBL4528465 1 -
CHEMBL4564188 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL254328 ABIRATERONE IC50 = 48.0 nM 7.32
CHEMBL2105738 GALETERONE IC50 = 140.0 nM 6.85
CHEMBL4591875 IC50 = 480.0 nM 6.32
CHEMBL4552506 IC50 = 25900.0 nM 4.59
CHEMBL4521939 IC50 = 39000.0 nM 4.41
CHEMBL1082407 ENZALUTAMIDE IC50 - -
CHEMBL4541575 IC50 > 15000.0 nM -
CHEMBL4581336 IC50 - -
CHEMBL4593419 IC50 - -
CHEMBL4532487 IC50 - -
CHEMBL4520316 IC50 - -
CHEMBL4539707 IC50 - -
CHEMBL4588643 IC50 - -
CHEMBL4528465 IC50 > 15000.0 nM -
CHEMBL4564188 IC50 - -