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Assay Detail

CHEMBL4701902

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

Binding
Inhibition of human ERG by Q-patch assay
18
Total Activities
18
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

Identification of TNO155, an Allosteric SHP2 Inhibitor for the Treatment of Cancer.
LaMarche MJ,Acker M,Argintaru A,Bauer D,Boisclair J,Chan H,Chen CH,Chen YN,Chen Z,Deng Z,Dore M,Dunstan D,Fan J,Fekkes P,Firestone B,Fodor M,Garcia-Fortanet J,Fortin PD,Fridrich C,Giraldes J,Glick M,Grunenfelder D,Hao HX,Hentemann M,Ho S,Jouk A,Kang ZB,Karki R,Kato M,Keen N,Koenig R,LaBonte LR,Larrow J,Liu G,Liu S,Majumdar D,Mathieu S,Meyer MJ,Mohseni M,Ntaganda R,Palermo M,Perez L,Pu M,Ramsey T,Reilly J,Sarver P,Sellers WR,Sendzik M,Shultz MD,Slisz J,Slocum K,Smith T,Spence S,Stams T,Straub C,Tamez V,Toure BB,Towler C,Wang P,Wang H,Williams SL,Yang F,Yu B,Zhang JH,Zhu S
J Med Chem (2020) 63 : 13578 -13594
PubMed 32910655 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.24 5.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4754023 1 5.77
CHEMBL4789106 1 5.62
CHEMBL4762625 1 5.55
CHEMBL4060033 1 5.23
CHEMBL4755819 1 5.22
CHEMBL4746224 1 5.21
CHEMBL4763213 1 4.92
CHEMBL4750422 1 4.91
CHEMBL4756767 1 4.76
CHEMBL4743002 1 -
CHEMBL4740294 1 -
CHEMBL4747789 1 -
CHEMBL4778151 1 -
CHEMBL4797606 1 -
CHEMBL4784611 1 -
CHEMBL4795635 1 -
CHEMBL4650521 BATOPROTAFIB 2.0 1 -
CHEMBL4763856 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4754023 IC50 = 1700.0 nM 5.77
CHEMBL4789106 IC50 = 2400.0 nM 5.62
CHEMBL4762625 IC50 = 2800.0 nM 5.55
CHEMBL4060033 IC50 = 5900.0 nM 5.23
CHEMBL4755819 IC50 = 6000.0 nM 5.22
CHEMBL4746224 IC50 = 6100.0 nM 5.21
CHEMBL4763213 IC50 = 11900.0 nM 4.92
CHEMBL4750422 IC50 = 12300.0 nM 4.91
CHEMBL4756767 IC50 = 17400.0 nM 4.76
CHEMBL4743002 IC50 - -
CHEMBL4740294 IC50 > 25000.0 nM -
CHEMBL4747789 IC50 > 30000.0 nM -
CHEMBL4778151 IC50 - -
CHEMBL4797606 IC50 - -
CHEMBL4784611 IC50 > 30000.0 nM -
CHEMBL4795635 IC50 - -
CHEMBL4650521 BATOPROTAFIB IC50 > 30000.0 nM -
CHEMBL4763856 IC50 - -