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Assay Detail

CHEMBL4414124

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Binding
Inhibition of human ERG by Q-patch assay
15
Total Activities
15
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

Publication

Optimization of Fused Bicyclic Allosteric SHP2 Inhibitors.
Bagdanoff JT, Chen Z, Acker M, Chen YN, Chan H, Dore M, Firestone B, Fodor M, Fortanet J, Hentemann M, Kato M, Koenig R, LaBonte LR, Liu S, Mohseni M, Ntaganda R, Sarver P, Smith T, Sendzik M, Stams T, Spence S, Towler C, Wang H, Wang P, Williams SL, LaMarche MJ.
J Med Chem (2019) 62 : 1781 -1792
PubMed 30688462 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.37 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4475043 1 8.40
CHEMBL4475081 1 8.15
CHEMBL4469071 1 6.70
CHEMBL4437876 1 6.60
CHEMBL4455446 1 6.54
CHEMBL4459445 1 6.03
CHEMBL4539145 1 6.01
CHEMBL4461938 1 5.92
CHEMBL4450282 1 5.72
CHEMBL4471006 1 5.18
CHEMBL4439006 1 4.77
CHEMBL4452417 1 -
CHEMBL4539178 1 -
CHEMBL4436233 1 -
CHEMBL4570587 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4475043 IC50 = 4.0 nM 8.40
CHEMBL4475081 IC50 = 7.0 nM 8.15
CHEMBL4469071 IC50 = 200.0 nM 6.70
CHEMBL4437876 IC50 = 250.0 nM 6.60
CHEMBL4455446 IC50 = 290.0 nM 6.54
CHEMBL4459445 IC50 = 930.0 nM 6.03
CHEMBL4539145 IC50 = 980.0 nM 6.01
CHEMBL4461938 IC50 = 1200.0 nM 5.92
CHEMBL4450282 IC50 = 1900.0 nM 5.72
CHEMBL4471006 IC50 = 6600.0 nM 5.18
CHEMBL4439006 IC50 = 17000.0 nM 4.77
CHEMBL4452417 IC50 > 30000.0 nM -
CHEMBL4539178 IC50 > 30000.0 nM -
CHEMBL4436233 IC50 > 30000.0 nM -
CHEMBL4570587 IC50 > 30000.0 nM -