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Lck Kinase Inhibition Assay from Article 10.1021/jm060727j: "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 i"
Assay data:54 Active, 13 Activity ≤ 1 nM, 43 Activity ≤ 1 µM, 61 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Human SRC proto-oncogene, non-receptor tyrosine kinase (Src family)
Assay data:21 Active, 21 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Human Janus kinase 3 (Janus kinase (JakA) family)
Assay data:32 Active, 32 Tested
Human LCK proto-oncogene, Src family tyrosine kinase (Src family)
Assay data:22 Active, 22 Tested
Human BLK proto-oncogene, Src family tyrosine kinase (Src family)
Assay data:10 Active, 10 Tested
Human HCK proto-oncogene, Src family tyrosine kinase (Src family)
Assay data:5 Active, 5 Tested
Human FGR proto-oncogene, Src family tyrosine kinase (Src family)
Human FYN proto-oncogene, Src family tyrosine kinase (Src family)
Assay data:8 Active, 8 Tested
Antiproliferative activity against human PC3 cells after 72 hrs
Assay data:13 Active, 13 Activity ≤ 1 µM, 13 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
Antiproliferative activity against human K562 cells after 72 hrs
Assay data:13 Active, 3 Activity ≤ 1 nM, 13 Activity ≤ 1 µM, 13 Tested
Inhibition of FGFR1
Assay data:1 Activity ≤ 1 µM, 2 Tested
SummaryCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of Her2
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Inhibition of Her1
Assay data:2 Active, 1 Activity ≤ 1 µM, 2 Tested
Inhibition of Cdk2
Assay data:2 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of Lyn
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Inhibition of Yes
Assay data:2 Active, 1 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 2 Tested
Inhibition of Fyn
Assay data:2 Active, 2 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 2 Tested
Reduction of Freund's adjuvant- induced paw edema in Lewis rat at 3 mg/kg, po
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed Citation
Reduction of Freund's adjuvant induced paw edema in Lewis rat at 0.3 mg/kg, po
Oral bioavailability in rat at 10 mg/kg, iv and po
Assay data:1 Tested
SummaryPubMed Citation
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