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Assay Detail

CHEMBL925259

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Binding
Inhibition of phosphorylated-Kdr after 30 mins
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

Discovery of N-phenyl nicotinamides as potent inhibitors of Kdr.
Dominguez C, Smith L, Huang Q, Yuan C, Ouyang X, Cai L, Chen P, Kim J, Harvey T, Syed R, Kim TS, Tasker A, Wang L, Zhang M, Coxon A, Bready J, Starnes C, Chen D, Gan Y, Neervannan S, Kumar G, Polverino A, Kendall R.
Bioorg Med Chem Lett (2007) 17 : 6003 -6008
PubMed 17869515 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 7.51 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL401153 1 8.70
CHEMBL250482 1 8.70
CHEMBL250684 1 8.40
CHEMBL400512 1 8.10
CHEMBL249179 1 8.05
CHEMBL385178 1 8.00
CHEMBL101683 1 7.82
CHEMBL248781 1 7.77
CHEMBL400140 1 7.72
CHEMBL248976 1 7.64
CHEMBL248978 1 7.64
CHEMBL249192 1 7.54
CHEMBL249806 1 7.42
CHEMBL249611 1 7.16
CHEMBL399546 1 7.04
CHEMBL248980 1 6.97
CHEMBL248820 1 6.87
CHEMBL250665 1 6.85
CHEMBL249194 1 6.59
CHEMBL400101 1 6.50
CHEMBL250471 1 6.31
CHEMBL250472 1 -
CHEMBL400584 1 -
CHEMBL249599 1 -
CHEMBL400102 1 -
CHEMBL249606 1 -
CHEMBL403349 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL401153 Ki = 2.0 nM 8.70
CHEMBL250482 Ki = 2.0 nM 8.70
CHEMBL250684 Ki = 4.0 nM 8.40
CHEMBL400512 Ki = 8.0 nM 8.10
CHEMBL249179 Ki = 9.0 nM 8.05
CHEMBL385178 Ki = 10.0 nM 8.00
CHEMBL101683 Ki = 15.0 nM 7.82
CHEMBL248781 Ki = 17.0 nM 7.77
CHEMBL400140 Ki = 19.0 nM 7.72
CHEMBL248976 Ki = 23.0 nM 7.64
CHEMBL248978 Ki = 23.0 nM 7.64
CHEMBL249192 Ki = 29.0 nM 7.54
CHEMBL249806 Ki = 38.0 nM 7.42
CHEMBL249611 Ki = 70.0 nM 7.16
CHEMBL399546 Ki = 91.0 nM 7.04
CHEMBL248980 Ki = 106.0 nM 6.97
CHEMBL248820 Ki = 135.0 nM 6.87
CHEMBL250665 Ki = 140.0 nM 6.85
CHEMBL249194 Ki = 259.0 nM 6.59
CHEMBL400101 Ki = 320.0 nM 6.50
CHEMBL250471 Ki = 490.0 nM 6.31
CHEMBL250472 Ki > 10000.0 nM -
CHEMBL400584 Ki > 10000.0 nM -
CHEMBL249599 Ki > 6660.0 nM -
CHEMBL400102 Ki > 6660.0 nM -
CHEMBL249606 Ki > 20000.0 nM -
CHEMBL403349 Ki > 20000.0 nM -