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Assay Detail

CHEMBL4276238

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

Binding
Binding affinity to N-terminal avi-tagged BRM ATPase-SnAC domain (unknown origin) in absence of ADP by SPR assay
2
Total Activities
1
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Probable global transcription activator SNF2L2 (CHEMBL2362979)
Type SINGLE PROTEIN
Organism Homo sapiens

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
Kd 1 7.06 7.06
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4290675 2 7.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4290675 Kd = 87.0 nM 7.06
CHEMBL4290675 Activity - -