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Assay Detail

CHEMBL888276

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

Binding
Inhibition of VEGFR2
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Synthesis and evaluation of pyrazolo[3,4-b]pyridine CDK1 inhibitors as anti-tumor agents.
Lin R, Connolly PJ, Lu Y, Chiu G, Li S, Yu Y, Huang S, Li X, Emanuel SL, Middleton SA, Gruninger RH, Adams M, Fuentes-Pesquera AR, Greenberger LM.
Bioorg Med Chem Lett (2007) 17 : 4297 -4302
PubMed 17532631 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.14 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL400569 1 7.60
CHEMBL248712 1 7.00
CHEMBL249094 1 7.00
CHEMBL249096 1 6.96
CHEMBL249302 1 6.96
CHEMBL248713 1 6.82
CHEMBL400859 1 6.80
CHEMBL249502 1 6.42
CHEMBL248891 1 6.34
CHEMBL400749 1 6.19
CHEMBL249304 1 6.00
CHEMBL401064 1 6.00
CHEMBL249500 1 5.97
CHEMBL391437 1 5.84
CHEMBL249303 1 5.81
CHEMBL249518 1 5.80
CHEMBL249519 1 5.33
CHEMBL400858 1 5.00
CHEMBL251739 1 5.00
CHEMBL399042 1 4.00
CHEMBL249501 1 -
CHEMBL251740 1 -
CHEMBL249095 1 -
CHEMBL400568 1 -
CHEMBL400906 1 -
CHEMBL248890 1 -
CHEMBL429478 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL400569 IC50 = 25.0 nM 7.60
CHEMBL248712 IC50 = 100.0 nM 7.00
CHEMBL249094 IC50 = 100.0 nM 7.00
CHEMBL249096 IC50 = 110.0 nM 6.96
CHEMBL249302 IC50 = 110.0 nM 6.96
CHEMBL248713 IC50 = 150.0 nM 6.82
CHEMBL400859 IC50 = 160.0 nM 6.80
CHEMBL249502 IC50 = 380.0 nM 6.42
CHEMBL248891 IC50 = 460.0 nM 6.34
CHEMBL400749 IC50 = 640.0 nM 6.19
CHEMBL249304 IC50 = 1000.0 nM 6.00
CHEMBL401064 IC50 = 1000.0 nM 6.00
CHEMBL249500 IC50 = 1070.0 nM 5.97
CHEMBL391437 IC50 = 1460.0 nM 5.84
CHEMBL249303 IC50 = 1550.0 nM 5.81
CHEMBL249518 IC50 = 1600.0 nM 5.80
CHEMBL249519 IC50 = 4670.0 nM 5.33
CHEMBL400858 IC50 = 10000.0 nM 5.00
CHEMBL251739 IC50 = 10000.0 nM 5.00
CHEMBL399042 IC50 = 100000.0 nM 4.00
CHEMBL249501 IC50 > 10000.0 nM -
CHEMBL251740 IC50 > 100000.0 nM -
CHEMBL249095 IC50 > 100000.0 nM -
CHEMBL400568 IC50 - -
CHEMBL400906 IC50 > 100.0 nM -
CHEMBL248890 IC50 > 100000.0 nM -
CHEMBL429478 IC50 > 100.0 nM -