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Assay Detail

CHEMBL5738727

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

Binding
In vitro kinase inhibition assay: An in vitro kinase assay was performed to evaluate the kinase suppression activity of the most promising cytotoxic candidates 4b, 4j against four different receptor tyrosine kinases (RTKs) - namely epidermal growth factor receptor (EGFR), human epidermal growth factor receptor (HER2), vascular endothelial growth factor receptor-2 (VEGFR-2) and platelet-derived growth factor receptor (PDGFR). The activities of the examined compounds against EGFR, HER2, PDGFR-β, and VEGFR2 were in vitro tested using Abcam's Human In cell ELISA Kit (ab 126419) for EGFR, ADP-Glo TM Kinase Assay for Her2, PDGFR-β, active, recombinant protein expressed in Sf9 cells for VEGFR2 (KDR) Kinase Assay Kit Catalog No. 40325, respectively.
9
Total Activities
3
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Target

Platelet-derived growth factor receptor beta (CHEMBL1913)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tetrahydroquinoline derivatives and a process of preparation thereof
(2022)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 9.61 9.85
kon 3 - -
k_off 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5977738 3 9.85
CHEMBL1336 SORAFENIB 4.0 3 9.59
CHEMBL5881155 3 9.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5977738 IC50 = 0.14 nM 9.85
CHEMBL1336 SORAFENIB IC50 = 0.26 nM 9.59
CHEMBL5881155 IC50 = 0.42 nM 9.38
CHEMBL5881155 kon = - -
CHEMBL5881155 k_off = - s-1 -
CHEMBL5977738 kon = - -
CHEMBL5977738 k_off = - s-1 -
CHEMBL1336 SORAFENIB kon = - -
CHEMBL1336 SORAFENIB k_off = - s-1 -