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Assay Detail

CHEMBL945309

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Binding
Inhibition of SYK
24
Total Activities
24
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 SYK (CHEMBL2599)
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 21 7.43 8.40
IC50 3 7.93 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL511670 1 8.40
CHEMBL471424 1 8.30
CHEMBL509161 1 8.10
CHEMBL512345 1 8.10
CHEMBL512172 1 8.05
CHEMBL485731 1 8.00
CHEMBL511811 1 8.00
CHEMBL472478 1 7.85
CHEMBL475249 1 7.66
CHEMBL451450 1 7.64
CHEMBL470780 1 7.64
CHEMBL475254 1 7.58
CHEMBL512319 1 7.55
CHEMBL471727 1 7.50
CHEMBL486751 1 7.48
CHEMBL471901 1 7.39
CHEMBL470175 1 7.36
CHEMBL485730 1 7.30
CHEMBL453217 1 7.25
CHEMBL471819 1 7.09
CHEMBL471776 1 6.96
CHEMBL473229 1 6.68
CHEMBL513985 1 6.20
CHEMBL475570 1 5.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL511670 Ki = 4.0 nM 8.40
CHEMBL471424 IC50 = 5.0 nM 8.30
CHEMBL509161 Ki = 8.0 nM 8.10
CHEMBL512345 IC50 = 8.0 nM 8.10
CHEMBL512172 Ki = 9.0 nM 8.05
CHEMBL485731 Ki = 10.0 nM 8.00
CHEMBL511811 Ki = 10.0 nM 8.00
CHEMBL472478 Ki = 14.0 nM 7.85
CHEMBL475249 Ki = 22.0 nM 7.66
CHEMBL451450 Ki = 23.0 nM 7.64
CHEMBL470780 Ki = 23.0 nM 7.64
CHEMBL475254 Ki = 26.0 nM 7.58
CHEMBL512319 Ki = 28.0 nM 7.55
CHEMBL471727 Ki = 32.0 nM 7.50
CHEMBL486751 Ki = 33.0 nM 7.48
CHEMBL471901 IC50 = 41.0 nM 7.39
CHEMBL470175 Ki = 44.0 nM 7.36
CHEMBL485730 Ki = 50.0 nM 7.30
CHEMBL453217 Ki = 56.0 nM 7.25
CHEMBL471819 Ki = 82.0 nM 7.09
CHEMBL471776 Ki = 110.0 nM 6.96
CHEMBL473229 Ki = 210.0 nM 6.68
CHEMBL513985 Ki = 630.0 nM 6.20
CHEMBL475570 Ki = 1817.0 nM 5.74