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Assay Detail

CHEMBL841264

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

Binding
In vitro inhibition of murine Lck kinase.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Proto-oncogene tyrosine-protein kinase LCK (CHEMBL2480)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56(Lck).
Wityak J, Das J, Moquin RV, Shen Z, Lin J, Chen P, Doweyko AM, Pitt S, Pang S, Shen DR, Fang Q, de Fex HF, Schieven GL, Kanner SB, Barrish JC.
Bioorg Med Chem Lett (2003) 13 : 4007 -4010
PubMed 14592495 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.70 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL131346 1 7.16
CHEMBL338159 1 6.77
CHEMBL130719 1 6.50
CHEMBL128589 1 6.14
CHEMBL132399 1 4.61
CHEMBL336330 1 4.39
CHEMBL128568 1 4.34
CHEMBL130943 1 -
CHEMBL130075 1 -
CHEMBL131167 1 -
CHEMBL128795 1 -
CHEMBL128455 1 -
CHEMBL341026 1 -
CHEMBL334341 1 -
CHEMBL424450 1 -
CHEMBL336544 1 -
CHEMBL423516 1 -
CHEMBL338488 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL131346 IC50 = 70.0 nM 7.16
CHEMBL338159 IC50 = 170.0 nM 6.77
CHEMBL130719 IC50 = 320.0 nM 6.50
CHEMBL128589 IC50 = 720.0 nM 6.14
CHEMBL132399 IC50 = 24300.0 nM 4.61
CHEMBL336330 IC50 = 40300.0 nM 4.39
CHEMBL128568 IC50 = 45700.0 nM 4.34
CHEMBL130943 IC50 > 50000.0 nM -
CHEMBL130075 IC50 > 50000.0 nM -
CHEMBL131167 IC50 > 50000.0 nM -
CHEMBL128795 IC50 > 50000.0 nM -
CHEMBL128455 IC50 > 50000.0 nM -
CHEMBL341026 IC50 > 50000.0 nM -
CHEMBL334341 IC50 > 50000.0 nM -
CHEMBL424450 IC50 > 50000.0 nM -
CHEMBL336544 IC50 > 50000.0 nM -
CHEMBL423516 IC50 > 50000.0 nM -
CHEMBL338488 IC50 > 50000.0 nM -