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Assay Detail

CHEMBL864159

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Binding
Inhibition of Itk
ChEMBL ↗
46
Total Activities
46
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 ITK/TSK (CHEMBL2959) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.
Das J, Furch JA, Liu C, Moquin RV, Lin J, Spergel SH, McIntyre KW, Shuster DJ, O'Day KD, Penhallow B, Hung CY, Doweyko AM, Kamath A, Zhang H, Marathe P, Kanner SB, Lin TA, Dodd JH, Barrish JC, Wityak J.
Bioorg Med Chem Lett (2006) 16 : 3706 -3712
PubMed 16682193 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 46 6.72 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL208846 — — 1 8.22
CHEMBL209881 — — 1 8.15
CHEMBL379478 — — 1 8.15
CHEMBL210248 — — 1 8.15
CHEMBL211842 — — 1 8.05
CHEMBL211355 — — 1 7.92
CHEMBL209163 — — 1 7.85
CHEMBL210123 — — 1 7.82
CHEMBL379114 — — 1 7.75
CHEMBL208901 — — 1 7.72
CHEMBL209148 — — 1 7.72
CHEMBL211291 — — 1 7.70
CHEMBL210985 — — 1 7.54
CHEMBL208542 — — 1 7.52
CHEMBL209004 — — 1 7.52
CHEMBL210528 — — 1 7.47
CHEMBL384680 — — 1 7.47
CHEMBL380058 — — 1 7.33
CHEMBL206905 — — 1 7.22
CHEMBL211601 — — 1 7.08
CHEMBL210243 — — 1 7.05
CHEMBL382362 — — 1 7.02
CHEMBL209400 — — 1 6.68
CHEMBL211136 — — 1 6.60
CHEMBL210932 — — 1 6.58
CHEMBL209009 — — 1 6.54
CHEMBL377750 — — 1 6.50
CHEMBL377906 — — 1 6.43
CHEMBL373513 — — 1 6.22
CHEMBL212269 — — 1 6.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL208846 — IC50 = 6.0 nM 8.22
CHEMBL209881 — IC50 = 7.0 nM 8.15
CHEMBL210248 — IC50 = 7.0 nM 8.15
CHEMBL379478 — IC50 = 7.0 nM 8.15
CHEMBL211842 — IC50 = 9.0 nM 8.05
CHEMBL211355 — IC50 = 12.0 nM 7.92
CHEMBL209163 — IC50 = 14.0 nM 7.85
CHEMBL210123 — IC50 = 15.0 nM 7.82
CHEMBL379114 — IC50 = 18.0 nM 7.75
CHEMBL208901 — IC50 = 19.0 nM 7.72
CHEMBL209148 — IC50 = 19.0 nM 7.72
CHEMBL211291 — IC50 = 20.0 nM 7.70
CHEMBL210985 — IC50 = 29.0 nM 7.54
CHEMBL208542 — IC50 = 30.0 nM 7.52
CHEMBL209004 — IC50 = 30.0 nM 7.52
CHEMBL210528 — IC50 = 34.0 nM 7.47
CHEMBL384680 — IC50 = 34.0 nM 7.47
CHEMBL380058 — IC50 = 47.0 nM 7.33
CHEMBL206905 — IC50 = 60.0 nM 7.22
CHEMBL211601 — IC50 = 83.0 nM 7.08
CHEMBL210243 — IC50 = 90.0 nM 7.05
CHEMBL382362 — IC50 = 96.0 nM 7.02
CHEMBL209400 — IC50 = 210.0 nM 6.68
CHEMBL211136 — IC50 = 250.0 nM 6.60
CHEMBL210932 — IC50 = 260.0 nM 6.58
CHEMBL209009 — IC50 = 290.0 nM 6.54
CHEMBL377750 — IC50 = 320.0 nM 6.50
CHEMBL377906 — IC50 = 370.0 nM 6.43
CHEMBL373513 — IC50 = 600.0 nM 6.22
CHEMBL212269 — IC50 = 690.0 nM 6.16
CHEMBL273966 — IC50 = 820.0 nM 6.09
CHEMBL210735 — IC50 = 940.0 nM 6.03
CHEMBL211021 — IC50 = 930.0 nM 6.03
CHEMBL437495 — IC50 = 970.0 nM 6.01
CHEMBL205799 — IC50 = 1000.0 nM 6.00
CHEMBL210046 — IC50 = 1130.0 nM 5.95
CHEMBL426685 — IC50 = 2190.0 nM 5.66
CHEMBL209056 — IC50 = 3900.0 nM 5.41
CHEMBL210953 — IC50 = 6060.0 nM 5.22
CHEMBL208541 — IC50 = 7070.0 nM 5.15
CHEMBL210599 — IC50 = 19240.0 nM 4.72
CHEMBL377355 — IC50 = 22340.0 nM 4.65
CHEMBL211998 — IC50 = 34200.0 nM 4.47
CHEMBL380042 — IC50 = 46300.0 nM 4.33
CHEMBL208867 — IC50 > 25000.0 nM -
CHEMBL211035 — IC50 > 50000.0 nM -