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Assay Detail

CHEMBL1645659

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Binding
Inhibition of human ERG
4
Total Activities
4
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

Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases.
Gallant M, Beaulieu C, Berthelette C, Colucci J, Crackower MA, Dalton C, Denis D, Ducharme Y, Friesen RW, Guay D, Gervais FG, Hamel M, Houle R, Krawczyk CM, Kosjek B, Lau S, Leblanc Y, Lee EE, Levesque JF, Mellon C, Molinaro C, Mullet W, O'Neill GP, O'Shea P, Sawyer N, Sillaots S, Simard D, Slipetz D, Stocco R, Sørensen D, Truong VL, Wong E, Wu J, Zaghdane H, Wang Z.
Bioorg Med Chem Lett (2011) 21 : 288 -293
PubMed 21106375 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 4.46 4.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1643773 1 4.46
CHEMBL561132 MK-7246 1.0 1 -
CHEMBL1643783 1 -
CHEMBL1643789 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1643773 Ki = 35000.0 nM 4.46
CHEMBL561132 MK-7246 Ki > 39000.0 nM -
CHEMBL1643783 Ki > 60000.0 nM -
CHEMBL1643789 Ki > 60000.0 nM -