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Assay Detail

CHEMBL4275676

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

Binding
Inhibition of R1881-induced transcriptional activity of human AR V7 truncated mutant expressed in human PC3 cells harboring pGL3-ARR3tk-NLuc after 24 hrs by luciferase reporter gene assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Small molecule-induced degradation of the full length and V7 truncated variant forms of human androgen receptor.
Dalal K, Morin H, Ban F, Shepherd A, Fernandez M, Tam KJ, Li H, LeBlanc E, Lack N, Prinz H, Rennie PS, Cherkasov A.
Eur J Med Chem (2018) 157 : 1164 -1173
PubMed 30193215 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.00 5.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1210876 1 5.00
CHEMBL1210959 1 5.00
CHEMBL1210878 1 5.00
CHEMBL1210880 1 -
CHEMBL113332 1 -
CHEMBL4278637 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1210876 IC50 = 10000.0 nM 5.00
CHEMBL1210959 IC50 = 10000.0 nM 5.00
CHEMBL1210878 IC50 = 10000.0 nM 5.00
CHEMBL1210880 IC50 > 10000.0 nM -
CHEMBL113332 IC50 < 10000.0 nM -
CHEMBL4278637 IC50 < 10000.0 nM -