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Assay Detail

CHEMBL910552

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Binding
Inhibition of human Lck in presence of ATP
ChEMBL ↗
53
Total Activities
53
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Tyrosine-protein kinase Lck (CHEMBL258) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

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 53 7.28 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL386118 — — 1 9.70
CHEMBL405630 — — 1 9.52
CHEMBL5416410 DASATINIB 4.0 1 9.40
CHEMBL186568 — — 1 9.30
CHEMBL273250 — — 1 9.30
CHEMBL189649 — — 1 9.30
CHEMBL365505 — — 1 9.22
CHEMBL216240 — — 1 9.15
CHEMBL214617 — — 1 9.15
CHEMBL364623 — — 1 9.00
CHEMBL189776 — — 1 8.92
CHEMBL386745 — — 1 8.92
CHEMBL217039 — — 1 8.89
CHEMBL384307 — — 1 8.52
CHEMBL407005 — — 1 8.40
CHEMBL188478 — — 1 8.40
CHEMBL385172 — — 1 8.31
CHEMBL386371 — — 1 8.30
CHEMBL384545 — — 1 8.20
CHEMBL189675 — — 1 8.17
CHEMBL360810 — — 1 8.03
CHEMBL386167 — — 1 7.77
CHEMBL131346 — — 1 7.52
CHEMBL131577 — — 1 7.46
CHEMBL186564 — — 1 7.30
CHEMBL384822 — — 1 6.89
CHEMBL215630 — — 1 6.89
CHEMBL217195 — — 1 6.80
CHEMBL217565 — — 1 6.75
CHEMBL338159 — — 1 6.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL386118 — IC50 = 0.2 nM 9.70
CHEMBL405630 — IC50 = 0.3 nM 9.52
CHEMBL5416410 DASATINIB IC50 = 0.4 nM 9.40
CHEMBL186568 — IC50 = 0.5 nM 9.30
CHEMBL273250 — IC50 = 0.5 nM 9.30
CHEMBL189649 — IC50 = 0.5 nM 9.30
CHEMBL365505 — IC50 = 0.6 nM 9.22
CHEMBL216240 — IC50 = 0.7 nM 9.15
CHEMBL214617 — IC50 = 0.7 nM 9.15
CHEMBL364623 — IC50 = 1.0 nM 9.00
CHEMBL189776 — IC50 = 1.2 nM 8.92
CHEMBL386745 — IC50 = 1.2 nM 8.92
CHEMBL217039 — IC50 = 1.3 nM 8.89
CHEMBL384307 — IC50 = 3.0 nM 8.52
CHEMBL188478 — IC50 = 4.0 nM 8.40
CHEMBL407005 — IC50 = 4.0 nM 8.40
CHEMBL385172 — IC50 = 4.9 nM 8.31
CHEMBL386371 — IC50 = 5.0 nM 8.30
CHEMBL384545 — IC50 = 6.3 nM 8.20
CHEMBL189675 — IC50 = 6.7 nM 8.17
CHEMBL360810 — IC50 = 9.4 nM 8.03
CHEMBL386167 — IC50 = 17.0 nM 7.77
CHEMBL131346 — IC50 = 30.0 nM 7.52
CHEMBL131577 — IC50 = 35.0 nM 7.46
CHEMBL186564 — IC50 = 50.0 nM 7.30
CHEMBL384822 — IC50 = 130.0 nM 6.89
CHEMBL215630 — IC50 = 130.0 nM 6.89
CHEMBL217195 — IC50 = 160.0 nM 6.80
CHEMBL217565 — IC50 = 180.0 nM 6.75
CHEMBL338159 — IC50 = 240.0 nM 6.62
CHEMBL131661 — IC50 = 360.0 nM 6.44
CHEMBL217486 — IC50 = 390.0 nM 6.41
CHEMBL214028 — IC50 = 480.0 nM 6.32
CHEMBL130160 — IC50 = 620.0 nM 6.21
CHEMBL128589 — IC50 = 700.0 nM 6.16
CHEMBL127500 — IC50 = 710.0 nM 6.15
CHEMBL130719 — IC50 = 800.0 nM 6.10
CHEMBL131393 — IC50 = 890.0 nM 6.05
CHEMBL217506 — IC50 = 1200.0 nM 5.92
CHEMBL216448 — IC50 = 1300.0 nM 5.89
CHEMBL408027 — IC50 = 1340.0 nM 5.87
CHEMBL340322 — IC50 = 1400.0 nM 5.85
CHEMBL128377 — IC50 = 1400.0 nM 5.85
CHEMBL66109 — IC50 = 1500.0 nM 5.82
CHEMBL217507 — IC50 = 2230.0 nM 5.65
CHEMBL129454 — IC50 = 4400.0 nM 5.36
CHEMBL337985 — IC50 = 4470.0 nM 5.35
CHEMBL307976 — IC50 = 5000.0 nM 5.30
CHEMBL385191 — IC50 = 12080.0 nM 4.92
CHEMBL132448 — IC50 = 12500.0 nM 4.90