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Assay Detail

CHEMBL992543

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

Binding
Inhibition of recombinant ITK by DELFIA assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Tyrosine-protein kinase ITK/TSK (CHEMBL2959)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Itk kinase inhibitors: initial efforts to improve the metabolical stability and the cell activity of the benzimidazole lead.
Moriarty KJ, Winters M, Qiao L, Ryan D, DesJarlis R, Robinson D, Cook BN, Kashem MA, Kaplita PV, Liu LH, Farrell TM, Khine HH, King J, Pullen SS, Roth GP, Magolda R, Takahashi H.
Bioorg Med Chem Lett (2008) 18 : 5537 -5540
PubMed 18819794 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 7.91 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL483581 1 8.70
CHEMBL460824 1 8.52
CHEMBL485202 1 8.52
CHEMBL485556 1 8.40
CHEMBL485030 1 8.40
CHEMBL485203 1 8.22
CHEMBL485626 1 8.15
CHEMBL462301 1 8.15
CHEMBL519033 1 8.10
CHEMBL457706 1 8.10
CHEMBL458796 1 8.00
CHEMBL460389 1 8.00
CHEMBL484945 1 8.00
CHEMBL484766 1 7.92
CHEMBL457886 1 7.85
CHEMBL462514 1 7.75
CHEMBL457705 1 7.64
CHEMBL517901 1 7.57
CHEMBL485201 1 7.57
CHEMBL490269 1 7.46
CHEMBL485584 1 7.27
CHEMBL485206 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL483581 IC50 = 2.0 nM 8.70
CHEMBL460824 IC50 = 3.0 nM 8.52
CHEMBL485202 IC50 = 3.0 nM 8.52
CHEMBL485556 IC50 = 4.0 nM 8.40
CHEMBL485030 IC50 = 4.0 nM 8.40
CHEMBL485203 IC50 = 6.0 nM 8.22
CHEMBL485626 IC50 = 7.0 nM 8.15
CHEMBL462301 IC50 = 7.0 nM 8.15
CHEMBL519033 IC50 = 8.0 nM 8.10
CHEMBL457706 IC50 = 8.0 nM 8.10
CHEMBL458796 IC50 = 10.0 nM 8.00
CHEMBL460389 IC50 = 10.0 nM 8.00
CHEMBL484945 IC50 = 10.0 nM 8.00
CHEMBL484766 IC50 = 12.0 nM 7.92
CHEMBL457886 IC50 = 14.0 nM 7.85
CHEMBL462514 IC50 = 18.0 nM 7.75
CHEMBL457705 IC50 = 23.0 nM 7.64
CHEMBL517901 IC50 = 27.0 nM 7.57
CHEMBL485201 IC50 = 27.0 nM 7.57
CHEMBL490269 IC50 = 35.0 nM 7.46
CHEMBL485584 IC50 = 54.0 nM 7.27
CHEMBL485206 IC50 = 1900.0 nM 5.72