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Assay Detail

CHEMBL3881022

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

Binding
Inhibition of unphosphorylated human 50 residues truncated cytoplasmic domain of VEGFR2 E990V mutant expressed in baculovirus/insect expression system assessed as reduction in NADH oxidation using poly(E4Y1) as substrate by pyruvate kinase/lactate dehydrogenase coupled assay
ChEMBL ↗
100
Total Activities
100
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

Indazole compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use
(2003)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 100 9.08 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3925855 — — 1 10.70
CHEMBL3915607 — — 1 10.52
CHEMBL3898789 — — 1 10.52
CHEMBL3915544 — — 1 10.40
CHEMBL3899609 — — 1 10.40
CHEMBL3545335 AG-13958 2.0 1 10.40
CHEMBL3952496 — — 1 10.34
CHEMBL3969695 — — 1 10.30
CHEMBL3891895 — — 1 10.22
CHEMBL3904168 — — 1 10.22
CHEMBL3984370 — — 1 10.21
CHEMBL3912174 — — 1 10.10
CHEMBL3889841 — — 1 10.10
CHEMBL3954818 — — 1 10.10
CHEMBL3894732 — — 1 10.03
CHEMBL3891135 — — 1 10.00
CHEMBL3960830 — — 1 9.96
CHEMBL3959310 — — 1 9.96
CHEMBL3978730 — — 1 9.96
CHEMBL3967940 — — 1 9.96
CHEMBL3930485 — — 1 9.89
CHEMBL3972140 — — 1 9.85
CHEMBL3956824 — — 1 9.74
CHEMBL3915626 — — 1 9.70
CHEMBL3891979 — — 1 9.66
CHEMBL3966821 — — 1 9.66
CHEMBL3914057 — — 1 9.66
CHEMBL3899200 — — 1 9.66
CHEMBL3922242 — — 1 9.64
CHEMBL3919150 — — 1 9.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3925855 — Ki = 0.02 nM 10.70
CHEMBL3915607 — Ki = 0.03 nM 10.52
CHEMBL3898789 — Ki = 0.03 nM 10.52
CHEMBL3915544 — Ki = 0.04 nM 10.40
CHEMBL3899609 — Ki = 0.04 nM 10.40
CHEMBL3545335 AG-13958 Ki = 0.04 nM 10.40
CHEMBL3952496 — Ki = 0.046 nM 10.34
CHEMBL3969695 — Ki = 0.05 nM 10.30
CHEMBL3891895 — Ki = 0.06 nM 10.22
CHEMBL3904168 — Ki = 0.06 nM 10.22
CHEMBL3984370 — Ki = 0.062 nM 10.21
CHEMBL3912174 — Ki = 0.08 nM 10.10
CHEMBL3889841 — Ki = 0.08 nM 10.10
CHEMBL3954818 — Ki = 0.08 nM 10.10
CHEMBL3894732 — Ki = 0.093 nM 10.03
CHEMBL3891135 — Ki = 0.1 nM 10.00
CHEMBL3960830 — Ki = 0.11 nM 9.96
CHEMBL3959310 — Ki = 0.11 nM 9.96
CHEMBL3978730 — Ki = 0.11 nM 9.96
CHEMBL3967940 — Ki = 0.11 nM 9.96
CHEMBL3930485 — Ki = 0.13 nM 9.89
CHEMBL3972140 — Ki = 0.14 nM 9.85
CHEMBL3956824 — Ki = 0.18 nM 9.74
CHEMBL3915626 — Ki = 0.2 nM 9.70
CHEMBL3899200 — Ki = 0.22 nM 9.66
CHEMBL3966821 — Ki = 0.22 nM 9.66
CHEMBL3891979 — Ki = 0.22 nM 9.66
CHEMBL3914057 — Ki = 0.22 nM 9.66
CHEMBL3922242 — Ki = 0.23 nM 9.64
CHEMBL3919150 — Ki = 0.25 nM 9.60
CHEMBL3956618 — Ki = 0.26 nM 9.59
CHEMBL3965764 — Ki = 0.27 nM 9.57
CHEMBL3963347 — Ki = 0.28 nM 9.55
CHEMBL3921873 — Ki = 0.29 nM 9.54
CHEMBL3923888 — Ki = 0.3 nM 9.52
CHEMBL3922509 — Ki = 0.33 nM 9.48
CHEMBL3951790 — Ki = 0.34 nM 9.47
CHEMBL3954085 — Ki = 0.35 nM 9.46
CHEMBL3925024 — Ki = 0.37 nM 9.43
CHEMBL3925826 — Ki = 0.37 nM 9.43
CHEMBL3982880 — Ki = 0.37 nM 9.43
CHEMBL3896103 — Ki = 0.39 nM 9.41
CHEMBL3906996 — Ki = 0.43 nM 9.37
CHEMBL3944307 — Ki = 0.48 nM 9.32
CHEMBL3941907 — Ki = 0.49 nM 9.31
CHEMBL3945318 — Ki = 0.54 nM 9.27
CHEMBL3963146 — Ki = 0.6 nM 9.22
CHEMBL3915043 — Ki = 0.63 nM 9.20
CHEMBL3947822 — Ki = 0.64 nM 9.19
CHEMBL3961315 — Ki = 0.65 nM 9.19