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Assay Detail

CHEMBL4276233

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

Binding
Inhibition of recombinant His10-tagged ZZ-HCV3C-BRM ATPase-SnAC (636 to 1331 residues) (unknown origin) expressed in insect sf9 cells preincubated for 5 mins followed by pCMV-dR8.91 plasmid and ATP addition measured after 60 mins by ADP-Glo assay
14
Total Activities
14
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

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
IC50 14 6.89 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4278436 1 8.30
CHEMBL4294655 1 8.00
CHEMBL4286757 1 7.48
CHEMBL4290175 1 7.22
CHEMBL4279505 1 6.96
CHEMBL4281368 1 6.70
CHEMBL4282784 1 6.01
CHEMBL4290675 1 5.96
CHEMBL4292870 1 5.42
CHEMBL4295096 1 -
CHEMBL4282980 1 -
CHEMBL4293567 1 -
CHEMBL4286345 1 -
CHEMBL4291666 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4278436 IC50 = 5.0 nM 8.30
CHEMBL4294655 IC50 = 10.0 nM 8.00
CHEMBL4286757 IC50 = 33.0 nM 7.48
CHEMBL4290175 IC50 = 60.0 nM 7.22
CHEMBL4279505 IC50 = 110.0 nM 6.96
CHEMBL4281368 IC50 = 200.0 nM 6.70
CHEMBL4282784 IC50 = 970.0 nM 6.01
CHEMBL4290675 IC50 = 1100.0 nM 5.96
CHEMBL4292870 IC50 = 3800.0 nM 5.42
CHEMBL4295096 IC50 < 5.0 nM -
CHEMBL4282980 IC50 < 5.0 nM -
CHEMBL4293567 IC50 < 5.0 nM -
CHEMBL4286345 IC50 < 5.0 nM -
CHEMBL4291666 IC50 > 50000.0 nM -