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Assay Detail

CHEMBL4357707

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

Binding
Inhibition of tracer 222 binding to recombinant human His-tagged TAK1 (437 to 504 residues) expressed in baculovirus expression system using tyrosine-4 peptide as substrate incubated for 60 mins by Lanthascreen assay
9
Total Activities
9
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

Target

Mitogen-activated protein kinase kinase kinase 7 (CHEMBL5776)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Based Design of a Potent and Selective Covalent Inhibitor for SRC Kinase That Targets a P-Loop Cysteine.
Du G, Rao S, Gurbani D, Henning NJ, Jiang J, Che J, Yang A, Ficarro SB, Marto JA, Aguirre AJ, Sorger PK, Westover KD, Zhang T, Gray NS.
J Med Chem (2020) 63 : 1624 -1641
PubMed 31935084 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.17 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3883384 1 7.30
CHEMBL4538743 1 6.65
CHEMBL4574265 1 6.26
CHEMBL4562024 1 5.83
CHEMBL4563120 1 5.72
CHEMBL4442889 1 5.26
CHEMBL4569421 1 -
CHEMBL4462060 1 -
CHEMBL4460150 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3883384 IC50 = 50.0 nM 7.30
CHEMBL4538743 IC50 = 224.0 nM 6.65
CHEMBL4574265 IC50 = 543.0 nM 6.26
CHEMBL4562024 IC50 = 1490.0 nM 5.83
CHEMBL4563120 IC50 = 1890.0 nM 5.72
CHEMBL4442889 IC50 = 5460.0 nM 5.26
CHEMBL4569421 IC50 - -
CHEMBL4462060 IC50 - -
CHEMBL4460150 IC50 - -