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Assay Detail

CHEMBL4479399

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

Binding
Inhibition of DHT-induced androgen receptor transactivation in human LNCaP cells after 24 hrs by luciferase reporter gene assay relative to control
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Androgen receptor (CHEMBL1871)
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
EC50 5 6.40 6.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1082407 ENZALUTAMIDE 4.0 1 6.75
CHEMBL4591875 1 6.72
CHEMBL4539707 1 6.33
CHEMBL4541575 1 5.78
CHEMBL4532487 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1082407 ENZALUTAMIDE EC50 = 180.0 nM 6.75
CHEMBL4591875 EC50 = 190.0 nM 6.72
CHEMBL4539707 EC50 = 470.0 nM 6.33
CHEMBL4541575 EC50 = 1650.0 nM 5.78
CHEMBL4532487 EC50 > 100.0 nM -