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Assay Detail

CHEMBL869847

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

Binding
Inhibition of KDR at 1 mM ATP by HTRF assay
50
Total Activities
50
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

1,4-Dihydroindeno[1,2-c]pyrazoles as novel multitargeted receptor tyrosine kinase inhibitors.
Dinges J, Ashworth KL, Akritopoulou-Zanze I, Arnold LD, Baumeister SA, Bousquet PF, Cunha GA, Davidsen SK, Djuric SW, Gracias VJ, Michaelides MR, Rafferty P, Sowin TJ, Stewart KD, Xia Z, Zhang HQ.
Bioorg Med Chem Lett (2006) 16 : 4266 -4271
PubMed 16759855 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 50 6.81 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL213910 1 7.96
CHEMBL378831 1 7.92
CHEMBL384294 1 7.80
CHEMBL212932 1 7.77
CHEMBL215948 1 7.75
CHEMBL211464 1 7.72
CHEMBL378895 1 7.70
CHEMBL380243 1 7.68
CHEMBL214063 1 7.68
CHEMBL379088 1 7.57
CHEMBL212986 1 7.47
CHEMBL380068 1 7.46
CHEMBL378440 1 7.38
CHEMBL213430 1 7.35
CHEMBL214161 1 7.32
CHEMBL223220 1 7.29
CHEMBL213507 1 7.21
CHEMBL209919 1 7.20
CHEMBL380397 1 7.10
CHEMBL211307 1 6.99
CHEMBL2096839 1 6.98
CHEMBL377400 1 6.91
CHEMBL209421 1 6.91
CHEMBL212084 1 6.83
CHEMBL225248 1 6.80
CHEMBL212985 1 6.80
CHEMBL210070 1 6.79
CHEMBL213270 1 6.77
CHEMBL213743 1 6.75
CHEMBL215563 1 6.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL213910 IC50 = 11.0 nM 7.96
CHEMBL378831 IC50 = 12.0 nM 7.92
CHEMBL384294 IC50 = 16.0 nM 7.80
CHEMBL212932 IC50 = 17.0 nM 7.77
CHEMBL215948 IC50 = 18.0 nM 7.75
CHEMBL211464 IC50 = 19.0 nM 7.72
CHEMBL378895 IC50 = 20.0 nM 7.70
CHEMBL380243 IC50 = 21.0 nM 7.68
CHEMBL214063 IC50 = 21.0 nM 7.68
CHEMBL379088 IC50 = 27.0 nM 7.57
CHEMBL212986 IC50 = 34.0 nM 7.47
CHEMBL380068 IC50 = 35.0 nM 7.46
CHEMBL378440 IC50 = 42.0 nM 7.38
CHEMBL213430 IC50 = 45.0 nM 7.35
CHEMBL214161 IC50 = 48.0 nM 7.32
CHEMBL223220 IC50 = 51.0 nM 7.29
CHEMBL213507 IC50 = 61.0 nM 7.21
CHEMBL209919 IC50 = 63.0 nM 7.20
CHEMBL380397 IC50 = 79.0 nM 7.10
CHEMBL211307 IC50 = 102.0 nM 6.99
CHEMBL2096839 IC50 = 104.0 nM 6.98
CHEMBL377400 IC50 = 123.0 nM 6.91
CHEMBL209421 IC50 = 122.0 nM 6.91
CHEMBL212084 IC50 = 147.0 nM 6.83
CHEMBL212985 IC50 = 159.0 nM 6.80
CHEMBL225248 IC50 = 159.0 nM 6.80
CHEMBL210070 IC50 = 164.0 nM 6.79
CHEMBL213270 IC50 = 171.0 nM 6.77
CHEMBL213743 IC50 = 180.0 nM 6.75
CHEMBL215563 IC50 = 180.0 nM 6.75
CHEMBL209971 IC50 = 180.0 nM 6.75
CHEMBL210113 IC50 = 184.0 nM 6.74
CHEMBL209922 IC50 = 199.0 nM 6.70
CHEMBL212499 IC50 = 212.0 nM 6.67
CHEMBL214109 IC50 = 259.0 nM 6.59
CHEMBL213909 IC50 = 262.0 nM 6.58
CHEMBL212762 IC50 = 281.0 nM 6.55
CHEMBL415047 IC50 = 308.0 nM 6.51
CHEMBL425615 IC50 = 444.0 nM 6.35
CHEMBL213796 IC50 = 459.0 nM 6.34
CHEMBL213138 IC50 = 2777.0 nM 5.56
CHEMBL215417 IC50 = 2882.0 nM 5.54
CHEMBL425262 IC50 = 4807.0 nM 5.32
CHEMBL212987 IC50 = 7458.0 nM 5.13
CHEMBL211515 IC50 = 12285.0 nM 4.91
CHEMBL213230 IC50 = 22795.0 nM 4.64
CHEMBL384939 IC50 = 24158.0 nM 4.62
CHEMBL211567 IC50 > 50000.0 nM -
CHEMBL443835 IC50 > 50000.0 nM -
CHEMBL214214 IC50 > 50000.0 nM -