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Assay Detail

CHEMBL3783186

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

Binding
Inhibition of HCK (unknown origin) preincubated for 2 hrs followed by FRET peptide addition measured after 1 hr by Z-LYTE assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Tyrosine-protein kinase HCK (CHEMBL3234)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Narrow Spectrum Kinase Inhibitors: New Therapeutic Agents for the Treatment of COPD and Steroid-Resistant Asthma.
Onions ST, Ito K, Charron CE, Brown RJ, Colucci M, Frickel F, Hardy G, Joly K, King-Underwood J, Kizawa Y, Knowles I, Murray PJ, Novak A, Rani A, Rapeport G, Smith A, Strong P, Taddei DM, Williams JG.
J Med Chem (2016) 59 : 1727 -1746
PubMed 26800309 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 6.30 7.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3781532 1 7.58
CHEMBL3781687 1 7.58
CHEMBL3781102 1 7.29
CHEMBL3695568 JNJ-49095397 2.0 1 7.28
CHEMBL3781430 1 7.09
CHEMBL3780832 1 6.96
CHEMBL3780154 1 6.79
CHEMBL3780667 1 6.73
CHEMBL3781244 1 6.71
CHEMBL3781245 1 6.68
CHEMBL3780488 1 6.32
CHEMBL3780111 1 6.20
CHEMBL3781473 1 6.16
CHEMBL3781982 1 6.09
CHEMBL3781587 1 6.08
CHEMBL143134 1 6.04
CHEMBL3782036 1 5.95
CHEMBL3780714 1 5.67
CHEMBL3782009 1 5.49
CHEMBL336001 1 5.31
CHEMBL3781999 1 5.07
CHEMBL3780386 1 5.06
CHEMBL3780519 1 4.88
CHEMBL3781413 1 -
CHEMBL3780410 1 -
CHEMBL3780629 1 -
CHEMBL3780089 1 -
CHEMBL343227 1 -
CHEMBL3781528 1 -
CHEMBL103667 DORAMAPIMOD 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3781532 IC50 = 26.0 nM 7.58
CHEMBL3781687 IC50 = 26.0 nM 7.58
CHEMBL3781102 IC50 = 51.0 nM 7.29
CHEMBL3695568 JNJ-49095397 IC50 = 52.0 nM 7.28
CHEMBL3781430 IC50 = 82.0 nM 7.09
CHEMBL3780832 IC50 = 110.0 nM 6.96
CHEMBL3780154 IC50 = 164.0 nM 6.79
CHEMBL3780667 IC50 = 187.0 nM 6.73
CHEMBL3781244 IC50 = 197.0 nM 6.71
CHEMBL3781245 IC50 = 208.0 nM 6.68
CHEMBL3780488 IC50 = 482.0 nM 6.32
CHEMBL3780111 IC50 = 625.0 nM 6.20
CHEMBL3781473 IC50 = 692.0 nM 6.16
CHEMBL3781982 IC50 = 807.0 nM 6.09
CHEMBL3781587 IC50 = 829.0 nM 6.08
CHEMBL143134 IC50 = 901.0 nM 6.04
CHEMBL3782036 IC50 = 1117.0 nM 5.95
CHEMBL3780714 IC50 = 2141.0 nM 5.67
CHEMBL3782009 IC50 = 3221.0 nM 5.49
CHEMBL336001 IC50 = 4937.0 nM 5.31
CHEMBL3781999 IC50 = 8552.0 nM 5.07
CHEMBL3780386 IC50 = 8673.0 nM 5.06
CHEMBL3780519 IC50 = 13291.0 nM 4.88
CHEMBL3781413 IC50 > 15000.0 nM -
CHEMBL3780410 IC50 > 16000.0 nM -
CHEMBL3780629 IC50 > 16000.0 nM -
CHEMBL3780089 IC50 > 17000.0 nM -
CHEMBL343227 IC50 > 19000.0 nM -
CHEMBL3781528 IC50 > 19000.0 nM -
CHEMBL103667 DORAMAPIMOD IC50 > 19000.0 nM -