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Assay Detail

CHEMBL871626

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

Binding
Inhibitory concentration against human KDR kinase expressed in NIH3T3 cells with 4 uM Biotin-Ahx-AEEEYFFLFA-amide at ambient temperature for 1 hr
ChEMBL ↗
65
Total Activities
65
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type NIH3T3
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Thienopyrimidine ureas as novel and potent multitargeted receptor tyrosine kinase inhibitors.
Dai Y, Guo Y, Frey RR, Ji Z, Curtin ML, Ahmed AA, Albert DH, Arnold L, Arries SS, Barlozzari T, Bauch JL, Bouska JJ, Bousquet PF, Cunha GA, Glaser KB, Guo J, Li J, Marcotte PA, Marsh KC, Moskey MD, Pease LJ, Stewart KD, Stoll VS, Tapang P, Wishart N, Davidsen SK, Michaelides MR.
J Med Chem (2005) 48 : 6066 -6083
PubMed 16162008 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 65 7.02 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL196363 — — 1 8.52
CHEMBL382979 — — 1 8.52
CHEMBL371329 — — 1 8.22
CHEMBL425749 — — 1 7.96
CHEMBL371206 — — 1 7.92
CHEMBL370545 — — 1 7.89
CHEMBL198297 — — 1 7.82
CHEMBL197635 — — 1 7.77
CHEMBL535 SUNITINIB 4.0 1 7.75
CHEMBL197353 — — 1 7.72
CHEMBL371510 — — 1 7.72
CHEMBL371225 — — 1 7.58
CHEMBL366241 — — 1 7.58
CHEMBL372744 — — 1 7.47
CHEMBL371889 — — 1 7.47
CHEMBL371379 — — 1 7.47
CHEMBL382517 — — 1 7.46
CHEMBL197592 — — 1 7.44
CHEMBL381207 — — 1 7.35
CHEMBL195955 — — 1 7.34
CHEMBL197828 — — 1 7.30
CHEMBL369908 — — 1 7.28
CHEMBL198267 — — 1 7.28
CHEMBL370325 — — 1 7.28
CHEMBL196499 — — 1 7.28
CHEMBL196747 — — 1 7.27
CHEMBL196020 — — 1 7.26
CHEMBL199031 — — 1 7.21
CHEMBL198155 — — 1 7.19
CHEMBL365784 — — 1 7.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL196363 — IC50 = 3.0 nM 8.52
CHEMBL382979 — IC50 = 3.0 nM 8.52
CHEMBL371329 — IC50 = 6.0 nM 8.22
CHEMBL425749 — IC50 = 11.0 nM 7.96
CHEMBL371206 — IC50 = 12.0 nM 7.92
CHEMBL370545 — IC50 = 13.0 nM 7.89
CHEMBL198297 — IC50 = 15.0 nM 7.82
CHEMBL197635 — IC50 = 17.0 nM 7.77
CHEMBL535 SUNITINIB IC50 = 18.0 nM 7.75
CHEMBL197353 — IC50 = 19.0 nM 7.72
CHEMBL371510 — IC50 = 19.0 nM 7.72
CHEMBL371225 — IC50 = 26.0 nM 7.58
CHEMBL366241 — IC50 = 26.0 nM 7.58
CHEMBL371889 — IC50 = 34.0 nM 7.47
CHEMBL372744 — IC50 = 34.0 nM 7.47
CHEMBL371379 — IC50 = 34.0 nM 7.47
CHEMBL382517 — IC50 = 35.0 nM 7.46
CHEMBL197592 — IC50 = 36.0 nM 7.44
CHEMBL381207 — IC50 = 45.0 nM 7.35
CHEMBL195955 — IC50 = 46.0 nM 7.34
CHEMBL197828 — IC50 = 50.0 nM 7.30
CHEMBL369908 — IC50 = 53.0 nM 7.28
CHEMBL198267 — IC50 = 53.0 nM 7.28
CHEMBL370325 — IC50 = 52.0 nM 7.28
CHEMBL196499 — IC50 = 52.0 nM 7.28
CHEMBL196747 — IC50 = 54.0 nM 7.27
CHEMBL196020 — IC50 = 55.0 nM 7.26
CHEMBL199031 — IC50 = 61.0 nM 7.21
CHEMBL198155 — IC50 = 64.0 nM 7.19
CHEMBL365784 — IC50 = 69.0 nM 7.16
CHEMBL196615 — IC50 = 83.0 nM 7.08
CHEMBL372174 — IC50 = 96.0 nM 7.02
CHEMBL194366 — IC50 = 100.0 nM 7.00
CHEMBL371332 — IC50 = 100.0 nM 7.00
CHEMBL194270 — IC50 = 110.0 nM 6.96
CHEMBL445394 — IC50 = 110.0 nM 6.96
CHEMBL194236 — IC50 = 120.0 nM 6.92
CHEMBL371890 — IC50 = 130.0 nM 6.89
CHEMBL262468 — IC50 = 150.0 nM 6.82
CHEMBL381034 — IC50 = 160.0 nM 6.80
CHEMBL195964 — IC50 = 170.0 nM 6.77
CHEMBL372960 — IC50 = 170.0 nM 6.77
CHEMBL425387 — IC50 = 180.0 nM 6.75
CHEMBL363393 — IC50 = 180.0 nM 6.75
CHEMBL382112 — IC50 = 210.0 nM 6.68
CHEMBL194842 — IC50 = 210.0 nM 6.68
CHEMBL196636 — IC50 = 230.0 nM 6.64
CHEMBL438797 — IC50 = 260.0 nM 6.58
CHEMBL372755 — IC50 = 280.0 nM 6.55
CHEMBL195828 — IC50 = 290.0 nM 6.54