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Assay Detail

CHEMBL4338771

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

Binding
Inhibition of kinase tracer 178 binding to recombinant human His-tagged DDR1 expressed in baculovirus infected Sf9 cells incubated for 1 hr by TR-FRET based LanthaScreen Eu kinase binding assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Epithelial discoidin domain-containing receptor 1 (CHEMBL5319)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of VU6015929: A Selective Discoidin Domain Receptor 1/2 (DDR1/2) Inhibitor to Explore the Role of DDR1 in Antifibrotic Therapy.
Jeffries DE, Borza CM, Blobaum AL, Pozzi A, Lindsley CW.
ACS Med Chem Lett (2020) 11 : 29 -33
PubMed 31938459 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 8.04 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4439970 1 8.40
CHEMBL4539920 1 8.33
CHEMBL4467377 1 8.23
CHEMBL4546339 1 8.07
CHEMBL4447700 1 7.98
CHEMBL4584937 1 7.82
CHEMBL4483465 1 7.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4439970 IC50 = 3.97 nM 8.40
CHEMBL4539920 IC50 = 4.67 nM 8.33
CHEMBL4467377 IC50 = 5.89 nM 8.23
CHEMBL4546339 IC50 = 8.53 nM 8.07
CHEMBL4447700 IC50 = 10.5 nM 7.98
CHEMBL4584937 IC50 = 15.2 nM 7.82
CHEMBL4483465 IC50 = 36.4 nM 7.44