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Assay Detail

CHEMBL3887353

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

Binding
Kinase Activity: The compounds prepared in Examples were tested for inhibitory activity against FMS, DDR1 and DDR2 kinases using Kinase Screening and Profiling Service (Invitrogen, U.S.).
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Discoidin domain-containing receptor 2 (CHEMBL5122)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Thieno[3,2-D]pyrimidine derivatives having inhibitory activity for protein kinases
(2015)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.49 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3969260 1 8.30
CHEMBL3944137 1 8.00
CHEMBL3977543 BELVARAFENIB 2.0 1 7.36
CHEMBL3954810 1 7.03
CHEMBL3915720 1 6.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3969260 IC50 = 5.0 nM 8.30
CHEMBL3944137 IC50 = 10.0 nM 8.00
CHEMBL3977543 BELVARAFENIB IC50 = 44.0 nM 7.36
CHEMBL3954810 IC50 = 93.0 nM 7.03
CHEMBL3915720 IC50 = 181.0 nM 6.74