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Assay Detail

CHEMBL4841802

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

Binding
Inhibition of GST-6His tagged VEGFR2 (unknown origin) using biotin-aminohexyl-EEEEYFELVAKKKK-NH2 peptide substrate incubated for 90 mins by HTRF assay
ChEMBL ↗
49
Total Activities
49
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

Vascular endothelial growth factor receptor 2 (CHEMBL279) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of Diarylurea Inhibitors of the Cardiac-Specific Kinase TNNI3K by Designing Selectivity Against VEGFR2, p38α, and B-Raf.
Patterson JR, Graves AP, Stoy P, Cheung M, Desai TA, Fries H, Gatto GJ, Holt DA, Shewchuk L, Totoritis R, Wang L, Kallander LS.
J Med Chem (2021) 64 : 15651 -15670
PubMed 34699203 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 49 7.24 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4875220 — — 1 9.40
CHEMBL4845883 — — 1 8.89
CHEMBL4856992 — — 1 8.70
CHEMBL4869054 — — 1 8.60
CHEMBL4857556 — — 1 8.60
CHEMBL4867760 — — 1 8.49
CHEMBL4852364 — — 1 8.49
CHEMBL1992306 — — 1 8.40
CHEMBL4870490 — — 1 8.30
CHEMBL4863203 — — 1 8.20
CHEMBL4849349 — — 1 8.10
CHEMBL4868251 — — 1 8.00
CHEMBL4870768 — — 1 7.89
CHEMBL4864463 — — 1 7.80
CHEMBL4066096 — — 1 7.80
CHEMBL4877505 — — 1 7.72
CHEMBL1233853 — — 1 7.70
CHEMBL4850780 — — 1 7.60
CHEMBL4863580 — — 1 7.60
CHEMBL4861519 — — 1 7.50
CHEMBL4868391 — — 1 7.40
CHEMBL4873406 — — 1 7.30
CHEMBL4874491 — — 1 7.30
CHEMBL4856623 — — 1 7.30
CHEMBL4865373 — — 1 7.30
CHEMBL4859380 — — 1 7.20
CHEMBL4872243 — — 1 7.20
CHEMBL4871527 — — 1 7.10
CHEMBL4850964 — — 1 7.10
CHEMBL4867053 — — 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4875220 — IC50 = 0.4 nM 9.40
CHEMBL4845883 — IC50 = 1.3 nM 8.89
CHEMBL4856992 — IC50 = 2.0 nM 8.70
CHEMBL4869054 — IC50 = 2.5 nM 8.60
CHEMBL4857556 — IC50 = 2.5 nM 8.60
CHEMBL4867760 — IC50 = 3.2 nM 8.49
CHEMBL4852364 — IC50 = 3.2 nM 8.49
CHEMBL1992306 — IC50 = 4.0 nM 8.40
CHEMBL4870490 — IC50 = 5.0 nM 8.30
CHEMBL4863203 — IC50 = 6.3 nM 8.20
CHEMBL4849349 — IC50 = 7.9 nM 8.10
CHEMBL4868251 — IC50 = 10.0 nM 8.00
CHEMBL4870768 — IC50 = 13.0 nM 7.89
CHEMBL4864463 — IC50 = 16.0 nM 7.80
CHEMBL4066096 — IC50 = 16.0 nM 7.80
CHEMBL4877505 — IC50 = 19.0 nM 7.72
CHEMBL1233853 — IC50 = 20.0 nM 7.70
CHEMBL4850780 — IC50 = 25.0 nM 7.60
CHEMBL4863580 — IC50 = 25.0 nM 7.60
CHEMBL4861519 — IC50 = 32.0 nM 7.50
CHEMBL4868391 — IC50 = 40.0 nM 7.40
CHEMBL4865373 — IC50 = 50.0 nM 7.30
CHEMBL4856623 — IC50 = 50.0 nM 7.30
CHEMBL4873406 — IC50 = 50.0 nM 7.30
CHEMBL4874491 — IC50 = 50.0 nM 7.30
CHEMBL4859380 — IC50 = 63.0 nM 7.20
CHEMBL4872243 — IC50 = 63.0 nM 7.20
CHEMBL4871527 — IC50 = 79.0 nM 7.10
CHEMBL4850964 — IC50 = 79.0 nM 7.10
CHEMBL4867053 — IC50 = 130.0 nM 6.89
CHEMBL4870079 — IC50 = 130.0 nM 6.89
CHEMBL4875166 — IC50 = 160.0 nM 6.80
CHEMBL4847826 — IC50 = 200.0 nM 6.70
CHEMBL4857725 — IC50 = 320.0 nM 6.50
CHEMBL4865829 — IC50 = 320.0 nM 6.50
CHEMBL4859309 — IC50 = 320.0 nM 6.50
CHEMBL4854957 — IC50 = 320.0 nM 6.50
CHEMBL4859818 — IC50 = 400.0 nM 6.40
CHEMBL4876578 — IC50 = 400.0 nM 6.40
CHEMBL4869303 — IC50 = 400.0 nM 6.40
CHEMBL4856606 — IC50 = 400.0 nM 6.40
CHEMBL4855081 — IC50 = 800.0 nM 6.10
CHEMBL4868757 — IC50 = 1000.0 nM 6.00
CHEMBL4870044 — IC50 = 2000.0 nM 5.70
CHEMBL4850251 — IC50 = 2500.0 nM 5.60
CHEMBL4867552 — IC50 = 2500.0 nM 5.60
CHEMBL4873277 — IC50 = 3200.0 nM 5.50
CHEMBL4856147 — IC50 = 6300.0 nM 5.20
CHEMBL4864978 — IC50 > 10000.0 nM -