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Assay Detail

CHEMBL4276243

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

Binding
Inhibition of BRM/BRG1 mutant-dependant cell proliferation in human SKMEL5 cells after 6 days by celltiter-glo luminescent cell viability assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of Orally Active Inhibitors of Brahma Homolog (BRM)/SMARCA2 ATPase Activity for the Treatment of Brahma Related Gene 1 (BRG1)/SMARCA4-Mutant Cancers.
Papillon JPN, Nakajima K, Adair CD, Hempel J, Jouk AO, Karki RG, Mathieu S, Möbitz H, Ntaganda R, Smith T, Visser M, Hill SE, Hurtado FK, Chenail G, Bhang HC, Bric A, Xiang K, Bushold G, Gilbert T, Vattay A, Dooley J, Costa EA, Park I, Li A, Farley D, Lounkine E, Yue QK, Xie X, Zhu X, Kulathila R, King D, Hu T, Vulic K, Cantwell J, Luu C, Jagani Z.
J Med Chem (2018) 61 : 10155 -10172
PubMed 30339381 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 7.58 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4295096 1 8.40
CHEMBL4282980 1 8.30
CHEMBL4293567 1 7.89
CHEMBL4286345 1 7.89
CHEMBL4278436 1 7.51
CHEMBL4294655 1 6.89
CHEMBL4286757 1 6.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4295096 EC50 = 4.0 nM 8.40
CHEMBL4282980 EC50 = 5.0 nM 8.30
CHEMBL4293567 EC50 = 13.0 nM 7.89
CHEMBL4286345 EC50 = 13.0 nM 7.89
CHEMBL4278436 EC50 = 31.0 nM 7.51
CHEMBL4294655 EC50 = 130.0 nM 6.89
CHEMBL4286757 EC50 = 650.0 nM 6.19