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Assay Detail

CHEMBL942219

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Binding
Inhibition of ITK by DELPHIA
30
Total Activities
30
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

2-Aminobenzimidazoles as potent ITK antagonists: trans-stilbene-like moieties targeting the kinase specificity pocket.
Lo HY, Bentzien J, Fleck RW, Pullen SS, Khine HH, Woska JR, Kugler SZ, Kashem MA, Takahashi H.
Bioorg Med Chem Lett (2008) 18 : 6218 -6221
PubMed 18930400 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 7.71 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL500517 1 8.30
CHEMBL485922 1 8.30
CHEMBL519250 1 8.30
CHEMBL500349 1 8.22
CHEMBL486951 1 8.22
CHEMBL507769 1 8.22
CHEMBL487785 1 8.15
CHEMBL501661 1 8.15
CHEMBL488596 1 8.10
CHEMBL485936 1 8.05
CHEMBL280766 1 8.05
CHEMBL499247 1 8.05
CHEMBL487786 1 8.00
CHEMBL519239 1 7.96
CHEMBL487571 1 7.92
CHEMBL454220 1 7.89
CHEMBL457886 1 7.60
CHEMBL442826 1 7.52
CHEMBL485937 1 7.43
CHEMBL486147 1 7.41
CHEMBL504194 1 7.41
CHEMBL500583 1 7.38
CHEMBL444394 1 7.24
CHEMBL501963 1 7.23
CHEMBL519388 1 7.20
CHEMBL488397 1 7.19
CHEMBL501364 1 7.17
CHEMBL510587 1 7.12
CHEMBL510877 1 6.89
CHEMBL447132 1 6.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL500517 IC50 = 5.0 nM 8.30
CHEMBL485922 IC50 = 5.0 nM 8.30
CHEMBL519250 IC50 = 5.0 nM 8.30
CHEMBL500349 IC50 = 6.0 nM 8.22
CHEMBL486951 IC50 = 6.0 nM 8.22
CHEMBL507769 IC50 = 6.0 nM 8.22
CHEMBL487785 IC50 = 7.0 nM 8.15
CHEMBL501661 IC50 = 7.0 nM 8.15
CHEMBL488596 IC50 = 8.0 nM 8.10
CHEMBL485936 IC50 = 9.0 nM 8.05
CHEMBL280766 IC50 = 9.0 nM 8.05
CHEMBL499247 IC50 = 9.0 nM 8.05
CHEMBL487786 IC50 = 10.0 nM 8.00
CHEMBL519239 IC50 = 11.0 nM 7.96
CHEMBL487571 IC50 = 12.0 nM 7.92
CHEMBL454220 IC50 = 13.0 nM 7.89
CHEMBL457886 IC50 = 25.0 nM 7.60
CHEMBL442826 IC50 = 30.0 nM 7.52
CHEMBL485937 IC50 = 37.0 nM 7.43
CHEMBL486147 IC50 = 39.0 nM 7.41
CHEMBL504194 IC50 = 39.0 nM 7.41
CHEMBL500583 IC50 = 42.0 nM 7.38
CHEMBL444394 IC50 = 58.0 nM 7.24
CHEMBL501963 IC50 = 59.0 nM 7.23
CHEMBL519388 IC50 = 63.0 nM 7.20
CHEMBL488397 IC50 = 65.0 nM 7.19
CHEMBL501364 IC50 = 67.0 nM 7.17
CHEMBL510587 IC50 = 75.0 nM 7.12
CHEMBL510877 IC50 = 130.0 nM 6.89
CHEMBL447132 IC50 = 270.0 nM 6.57