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Assay Detail

CHEMBL992190

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

Binding
Inhibition of ITK by DELFIA method
ChEMBL ↗
47
Total Activities
47
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

Discovery of potent inhibitors of interleukin-2 inducible T-cell kinase (ITK) through structure-based drug design.
Cook BN, Bentzien J, White A, Nemoto PA, Wang J, Man CC, Soleymanzadeh F, Khine HH, Kashem MA, Kugler SZ, Wolak JP, Roth GP, De Lombaert S, Pullen SS, Takahashi H.
Bioorg Med Chem Lett (2009) 19 : 773 -777
PubMed 19111460 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 47 7.47 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL482169 — — 1 8.70
CHEMBL519960 — — 1 8.70
CHEMBL481884 — — 1 8.70
CHEMBL481720 — — 1 8.70
CHEMBL481900 — — 1 8.70
CHEMBL520110 — — 1 8.52
CHEMBL475593 — — 1 8.30
CHEMBL481378 — — 1 8.30
CHEMBL480754 — — 1 8.22
CHEMBL482367 — — 1 8.10
CHEMBL481738 — — 1 8.10
CHEMBL520432 — — 1 8.00
CHEMBL521113 — — 1 8.00
CHEMBL481559 — — 1 7.96
CHEMBL519927 — — 1 7.89
CHEMBL521432 — — 1 7.85
CHEMBL480573 — — 1 7.85
CHEMBL481379 — — 1 7.85
CHEMBL481380 — — 1 7.82
CHEMBL457706 — — 1 7.82
CHEMBL460824 — — 1 7.77
CHEMBL485203 — — 1 7.75
CHEMBL481721 — — 1 7.72
CHEMBL480554 — — 1 7.70
CHEMBL481361 — — 1 7.58
CHEMBL480574 — — 1 7.46
CHEMBL518937 — — 1 7.41
CHEMBL480555 — — 1 7.26
CHEMBL521241 — — 1 7.24
CHEMBL457886 — — 1 7.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL482169 — IC50 = 2.0 nM 8.70
CHEMBL481900 — IC50 = 2.0 nM 8.70
CHEMBL481720 — IC50 = 2.0 nM 8.70
CHEMBL519960 — IC50 = 2.0 nM 8.70
CHEMBL481884 — IC50 = 2.0 nM 8.70
CHEMBL520110 — IC50 = 3.0 nM 8.52
CHEMBL475593 — IC50 = 5.0 nM 8.30
CHEMBL481378 — IC50 = 5.0 nM 8.30
CHEMBL480754 — IC50 = 6.0 nM 8.22
CHEMBL482367 — IC50 = 8.0 nM 8.10
CHEMBL481738 — IC50 = 8.0 nM 8.10
CHEMBL520432 — IC50 = 10.0 nM 8.00
CHEMBL521113 — IC50 = 10.0 nM 8.00
CHEMBL481559 — IC50 = 11.0 nM 7.96
CHEMBL519927 — IC50 = 13.0 nM 7.89
CHEMBL521432 — IC50 = 14.0 nM 7.85
CHEMBL481379 — IC50 = 14.0 nM 7.85
CHEMBL480573 — IC50 = 14.0 nM 7.85
CHEMBL481380 — IC50 = 15.0 nM 7.82
CHEMBL457706 — IC50 = 15.0 nM 7.82
CHEMBL460824 — IC50 = 17.0 nM 7.77
CHEMBL485203 — IC50 = 18.0 nM 7.75
CHEMBL481721 — IC50 = 19.0 nM 7.72
CHEMBL480554 — IC50 = 20.0 nM 7.70
CHEMBL481361 — IC50 = 26.0 nM 7.58
CHEMBL480574 — IC50 = 35.0 nM 7.46
CHEMBL518937 — IC50 = 39.0 nM 7.41
CHEMBL480555 — IC50 = 55.0 nM 7.26
CHEMBL521241 — IC50 = 57.0 nM 7.24
CHEMBL457886 — IC50 = 58.0 nM 7.24
CHEMBL480753 — IC50 = 74.0 nM 7.13
CHEMBL481567 — IC50 = 81.0 nM 7.09
CHEMBL480374 — IC50 = 95.0 nM 7.02
CHEMBL458796 — IC50 = 100.0 nM 7.00
CHEMBL519116 — IC50 = 130.0 nM 6.89
CHEMBL480566 — IC50 = 140.0 nM 6.85
CHEMBL480592 — IC50 = 150.0 nM 6.82
CHEMBL480547 — IC50 = 170.0 nM 6.77
CHEMBL480365 — IC50 = 170.0 nM 6.77
CHEMBL485202 — IC50 = 180.0 nM 6.75
CHEMBL481360 — IC50 = 180.0 nM 6.75
CHEMBL481369 — IC50 = 340.0 nM 6.47
CHEMBL481901 — IC50 = 380.0 nM 6.42
CHEMBL481370 — IC50 = 450.0 nM 6.35
CHEMBL520768 — IC50 = 1000.0 nM 6.00
CHEMBL480373 — IC50 = 2500.0 nM 5.60
CHEMBL481362 — IC50 = 10000.0 nM 5.00