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Assay Detail

CHEMBL945313

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

Binding
Inhibition of ZAP70
20
Total Activities
20
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Tyrosine-protein kinase ZAP-70 (CHEMBL2803)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and SAR of novel 4-thiazolyl-2-phenylaminopyrimidines as potent inhibitors of spleen tyrosine kinase (SYK).
Farmer LJ, Bemis G, Britt SD, Cochran J, Connors M, Harrington EM, Hoock T, Markland W, Nanthakumar S, Taslimi P, Ter Haar E, Wang J, Zhaveri D, Salituro FG.
Bioorg Med Chem Lett (2008) 18 : 6231 -6235
PubMed 18938080 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 6.13 6.62
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL512172 1 6.62
CHEMBL511670 1 6.57
CHEMBL472478 1 6.50
CHEMBL470780 1 6.39
CHEMBL509161 1 6.38
CHEMBL511811 1 6.35
CHEMBL471727 1 6.25
CHEMBL485730 1 6.17
CHEMBL475254 1 6.17
CHEMBL470175 1 6.12
CHEMBL485731 1 6.12
CHEMBL471776 1 6.05
CHEMBL486751 1 6.00
CHEMBL453217 1 5.99
CHEMBL451450 1 5.94
CHEMBL473229 1 5.82
CHEMBL471819 1 5.81
CHEMBL512319 1 5.67
CHEMBL475249 1 5.46
CHEMBL475570 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL512172 Ki = 240.0 nM 6.62
CHEMBL511670 Ki = 270.0 nM 6.57
CHEMBL472478 Ki = 318.0 nM 6.50
CHEMBL470780 Ki = 410.0 nM 6.39
CHEMBL509161 Ki = 419.1 nM 6.38
CHEMBL511811 Ki = 450.0 nM 6.35
CHEMBL471727 Ki = 560.0 nM 6.25
CHEMBL485730 Ki = 680.0 nM 6.17
CHEMBL475254 Ki = 677.0 nM 6.17
CHEMBL470175 Ki = 754.0 nM 6.12
CHEMBL485731 Ki = 750.0 nM 6.12
CHEMBL471776 Ki = 891.0 nM 6.05
CHEMBL486751 Ki = 1000.0 nM 6.00
CHEMBL453217 Ki = 1030.0 nM 5.99
CHEMBL451450 Ki = 1140.0 nM 5.94
CHEMBL473229 Ki = 1500.0 nM 5.82
CHEMBL471819 Ki = 1551.0 nM 5.81
CHEMBL512319 Ki = 2145.0 nM 5.67
CHEMBL475249 Ki = 3500.0 nM 5.46
CHEMBL475570 Activity - -