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Assay Detail

CHEMBL805362

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

Binding
In vitro inhibition of Src protein tyrosine kinase using the Scintillation proximity kinase assay.
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Proto-oncogene tyrosine-protein kinase Src (CHEMBL267)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Bone-targeted Src kinase inhibitors: novel pyrrolo- and pyrazolopyrimidine analogues.
Sundaramoorthi R, Shakespeare WC, Keenan TP, Metcalf CA, Wang Y, Mani U, Taylor M, Liu S, Bohacek RS, Narula SS, Dalgarno DC, van Schravandijk MR, Violette SM, Liou S, Adams S, Ram MK, Keats JA, Weigle M, Sawyer TK, Weigele M.
Bioorg Med Chem Lett (2003) 13 : 3063 -3066
PubMed 12941334 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.38 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL318996 1 8.40
CHEMBL3706663 1 7.70
CHEMBL105056 1 7.40
CHEMBL102946 1 7.40
CHEMBL104215 1 7.22
CHEMBL321779 1 6.92
CHEMBL105436 1 6.80
CHEMBL104857 1 6.60
CHEMBL421025 1 6.51
CHEMBL3706661 1 6.50
CHEMBL321116 1 6.44
CHEMBL3706662 1 6.40
CHEMBL421405 1 6.17
CHEMBL102183 1 6.16
CHEMBL321569 1 6.06
CHEMBL320417 1 5.94
CHEMBL317693 1 5.82
CHEMBL3706664 1 5.80
CHEMBL105516 1 5.60
CHEMBL105005 1 5.40
CHEMBL104077 1 4.72
CHEMBL101795 1 4.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL318996 IC50 = 4.0 nM 8.40
CHEMBL3706663 IC50 = 20.0 nM 7.70
CHEMBL105056 IC50 = 40.0 nM 7.40
CHEMBL102946 IC50 = 40.0 nM 7.40
CHEMBL104215 IC50 = 60.0 nM 7.22
CHEMBL321779 IC50 = 120.0 nM 6.92
CHEMBL105436 IC50 = 160.0 nM 6.80
CHEMBL104857 IC50 = 250.0 nM 6.60
CHEMBL421025 IC50 = 310.0 nM 6.51
CHEMBL3706661 IC50 = 320.0 nM 6.50
CHEMBL321116 IC50 = 360.0 nM 6.44
CHEMBL3706662 IC50 = 400.0 nM 6.40
CHEMBL421405 IC50 = 680.0 nM 6.17
CHEMBL102183 IC50 = 700.0 nM 6.16
CHEMBL321569 IC50 = 870.0 nM 6.06
CHEMBL320417 IC50 = 1150.0 nM 5.94
CHEMBL317693 IC50 = 1500.0 nM 5.82
CHEMBL3706664 IC50 = 1600.0 nM 5.80
CHEMBL105516 IC50 = 2500.0 nM 5.60
CHEMBL105005 IC50 = 4000.0 nM 5.40
CHEMBL104077 IC50 = 19000.0 nM 4.72
CHEMBL101795 IC50 = 40000.0 nM 4.40