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Assay Detail

CHEMBL929949

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Binding
Inhibition of Lck
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Tyrosine-protein kinase Lck (CHEMBL258)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38alpha MAP kinase inhibitor.
Hynes J, Wu H, Pitt S, Shen DR, Zhang R, Schieven GL, Gillooly KM, Shuster DJ, Taylor TL, Yang X, McIntyre KW, McKinnon M, Zhang H, Marathe PH, Doweyko AM, Kish K, Kiefer SE, Sack JS, Newitt JA, Barrish JC, Dodd J, Leftheris K.
Bioorg Med Chem Lett (2008) 18 : 1762 -1767
PubMed 18313298 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.67 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL258403 1 6.85
CHEMBL403200 1 6.42
CHEMBL255482 1 5.72
CHEMBL255428 1 5.48
CHEMBL257996 1 5.32
CHEMBL258223 1 5.24
CHEMBL258202 1 4.66
CHEMBL255698 1 -
CHEMBL258203 1 -
CHEMBL258201 1 -
CHEMBL257995 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL258403 IC50 = 140.0 nM 6.85
CHEMBL403200 IC50 = 380.0 nM 6.42
CHEMBL255482 IC50 = 1900.0 nM 5.72
CHEMBL255428 IC50 = 3310.0 nM 5.48
CHEMBL257996 IC50 = 4800.0 nM 5.32
CHEMBL258223 IC50 = 5800.0 nM 5.24
CHEMBL258202 IC50 = 22000.0 nM 4.66
CHEMBL255698 IC50 > 50000.0 nM -
CHEMBL258203 IC50 > 50000.0 nM -
CHEMBL258201 IC50 > 50000.0 nM -
CHEMBL257995 IC50 > 50000.0 nM -