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Assay Detail

CHEMBL910553

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Functional
Inhibition of anti CD3/anti CD28-induced T cell proliferation
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type T-cell
Confidence 1 — Organism
Curated By Expert

Target

T-cell (CHEMBL614309)
Type CELL-LINE

Publication

2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor.
Das J, Chen P, Norris D, Padmanabha R, Lin J, Moquin RV, Shen Z, Cook LS, Doweyko AM, Pitt S, Pang S, Shen DR, Fang Q, de Fex HF, McIntyre KW, Shuster DJ, Gillooly KM, Behnia K, Schieven GL, Wityak J, Barrish JC.
J Med Chem (2006) 49 : 6819 -6832
PubMed 17154512 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 7.18 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL424906 1 8.70
CHEMBL5416410 DASATINIB 4.0 1 8.52
CHEMBL189649 1 8.52
CHEMBL216240 1 8.40
CHEMBL217039 1 8.30
CHEMBL214617 1 8.15
CHEMBL273250 1 8.10
CHEMBL386118 1 7.64
CHEMBL385698 1 7.12
CHEMBL186568 1 7.10
CHEMBL364623 1 7.10
CHEMBL365505 1 6.96
CHEMBL188478 1 6.85
CHEMBL189776 1 6.85
CHEMBL384307 1 6.85
CHEMBL386745 1 6.75
CHEMBL360810 1 6.57
CHEMBL405630 1 6.46
CHEMBL407005 1 6.46
CHEMBL385172 1 6.30
CHEMBL386371 1 6.29
CHEMBL384545 1 6.24
CHEMBL189675 1 6.06
CHEMBL131577 1 6.05
CHEMBL307976 1 -
CHEMBL386167 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL424906 IC50 = 2.0 nM 8.70
CHEMBL5416410 DASATINIB IC50 = 3.0 nM 8.52
CHEMBL189649 IC50 = 3.0 nM 8.52
CHEMBL216240 IC50 = 4.0 nM 8.40
CHEMBL217039 IC50 = 5.0 nM 8.30
CHEMBL214617 IC50 = 7.0 nM 8.15
CHEMBL273250 IC50 = 8.0 nM 8.10
CHEMBL386118 IC50 = 23.0 nM 7.64
CHEMBL385698 IC50 = 75.0 nM 7.12
CHEMBL186568 IC50 = 80.0 nM 7.10
CHEMBL364623 IC50 = 80.0 nM 7.10
CHEMBL365505 IC50 = 110.0 nM 6.96
CHEMBL188478 IC50 = 140.0 nM 6.85
CHEMBL189776 IC50 = 140.0 nM 6.85
CHEMBL384307 IC50 = 140.0 nM 6.85
CHEMBL386745 IC50 = 180.0 nM 6.75
CHEMBL360810 IC50 = 270.0 nM 6.57
CHEMBL405630 IC50 = 350.0 nM 6.46
CHEMBL407005 IC50 = 350.0 nM 6.46
CHEMBL385172 IC50 = 500.0 nM 6.30
CHEMBL386371 IC50 = 510.0 nM 6.29
CHEMBL384545 IC50 = 570.0 nM 6.24
CHEMBL189675 IC50 = 870.0 nM 6.06
CHEMBL131577 IC50 = 884.0 nM 6.05
CHEMBL307976 IC50 > 10000.0 nM -
CHEMBL386167 IC50 > 2000.0 nM -