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Assay Detail

CHEMBL841202

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

Binding
In vitro inhibition of phosphorylation of an exogenous substrate by human p56 Lck tyrosine kinase expressed as a His-tagged protein in insect cells using a baculovirus expression system
ChEMBL ↗
61
Total Activities
61
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Molecular design, synthesis, and structure-Activity relationships leading to the potent and selective p56(lck) inhibitor BMS-243117.
Das J, Lin J, Moquin RV, Shen Z, Spergel SH, Wityak J, Doweyko AM, DeFex HF, Fang Q, Pang S, Pitt S, Shen DR, Schieven GL, Barrish JC.
Bioorg Med Chem Lett (2003) 13 : 2145 -2149
PubMed 12798323 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 61 6.64 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL68871 — — 1 8.40
CHEMBL67237 — — 1 8.40
CHEMBL308432 — — 1 8.15
CHEMBL67758 — — 1 8.05
CHEMBL304146 — — 1 7.96
CHEMBL68352 — — 1 7.82
CHEMBL304300 — — 1 7.72
CHEMBL68411 — — 1 7.70
CHEMBL304559 — — 1 7.52
CHEMBL302140 — — 1 7.41
CHEMBL66990 — — 1 7.35
CHEMBL69481 — — 1 7.26
CHEMBL302073 — — 1 7.16
CHEMBL65835 — — 1 7.16
CHEMBL66283 — — 1 7.10
CHEMBL66014 — — 1 7.06
CHEMBL70035 — — 1 7.05
CHEMBL302119 — — 1 7.05
CHEMBL302308 — — 1 7.05
CHEMBL67167 — — 1 7.00
CHEMBL67558 — — 1 6.96
CHEMBL68104 — — 1 6.91
CHEMBL308684 — — 1 6.70
CHEMBL68398 — — 1 6.57
CHEMBL303686 — — 1 6.54
CHEMBL302336 — — 1 6.52
CHEMBL302108 — — 1 6.51
CHEMBL304789 — — 1 6.48
CHEMBL304399 — — 1 6.25
CHEMBL67292 — — 1 6.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL68871 — IC50 = 4.0 nM 8.40
CHEMBL67237 — IC50 = 4.0 nM 8.40
CHEMBL308432 — IC50 = 7.0 nM 8.15
CHEMBL67758 — IC50 = 9.0 nM 8.05
CHEMBL304146 — IC50 = 11.0 nM 7.96
CHEMBL68352 — IC50 = 15.0 nM 7.82
CHEMBL304300 — IC50 = 19.0 nM 7.72
CHEMBL68411 — IC50 = 20.0 nM 7.70
CHEMBL304559 — IC50 = 30.0 nM 7.52
CHEMBL302140 — IC50 = 39.0 nM 7.41
CHEMBL66990 — IC50 = 45.0 nM 7.35
CHEMBL69481 — IC50 = 55.0 nM 7.26
CHEMBL302073 — IC50 = 70.0 nM 7.16
CHEMBL65835 — IC50 = 70.0 nM 7.16
CHEMBL66283 — IC50 = 80.0 nM 7.10
CHEMBL66014 — IC50 = 87.0 nM 7.06
CHEMBL70035 — IC50 = 90.0 nM 7.05
CHEMBL302119 — IC50 = 90.0 nM 7.05
CHEMBL302308 — IC50 = 90.0 nM 7.05
CHEMBL67167 — IC50 = 100.0 nM 7.00
CHEMBL67558 — IC50 = 110.0 nM 6.96
CHEMBL68104 — IC50 = 123.0 nM 6.91
CHEMBL308684 — IC50 = 200.0 nM 6.70
CHEMBL68398 — IC50 = 272.0 nM 6.57
CHEMBL303686 — IC50 = 290.0 nM 6.54
CHEMBL302336 — IC50 = 300.0 nM 6.52
CHEMBL302108 — IC50 = 310.0 nM 6.51
CHEMBL304789 — IC50 = 330.0 nM 6.48
CHEMBL304399 — IC50 = 565.0 nM 6.25
CHEMBL67292 — IC50 = 666.0 nM 6.18
CHEMBL303244 — IC50 = 700.0 nM 6.16
CHEMBL305249 — IC50 = 1730.0 nM 5.76
CHEMBL304061 — IC50 = 1800.0 nM 5.75
CHEMBL305399 — IC50 = 2010.0 nM 5.70
CHEMBL66109 — IC50 = 3000.0 nM 5.52
CHEMBL67987 — IC50 = 3120.0 nM 5.51
CHEMBL307976 — IC50 = 3200.0 nM 5.50
CHEMBL65785 — IC50 = 3230.0 nM 5.49
CHEMBL67258 — IC50 = 4270.0 nM 5.37
CHEMBL69693 — IC50 = 4400.0 nM 5.36
CHEMBL308024 — IC50 = 5600.0 nM 5.25
CHEMBL65941 — IC50 = 7250.0 nM 5.14
CHEMBL66971 — IC50 = 15000.0 nM 4.82
CHEMBL303399 — IC50 = 23000.0 nM 4.64
CHEMBL70244 — IC50 > 12500.0 nM -
CHEMBL69601 — IC50 > 12500.0 nM -
CHEMBL304357 — IC50 > 3125.0 nM -
CHEMBL68645 — IC50 > 12500.0 nM -
CHEMBL69641 — IC50 > 12500.0 nM -
CHEMBL67467 — IC50 > 12500.0 nM -