Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL992567

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

Binding
Inhibition of IRK
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Insulin receptor (CHEMBL1981)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery, SAR and X-ray structure of 1H-benzimidazole-5-carboxylic acid cyclohexyl-methyl-amides as inhibitors of inducible T-cell kinase (Itk).
Moriarty KJ, Takahashi H, Pullen SS, Khine HH, Sallati RH, Raymond EL, Woska JR, Jeanfavre DD, Roth GP, Winters MP, Qiao L, Ryan D, DesJarlais R, Robinson D, Wilson M, Bobko M, Cook BN, Lo HY, Nemoto PA, Kashem MA, Wolak JP, White A, Magolda RL, Tomczuk B.
Bioorg Med Chem Lett (2008) 18 : 5545 -5549
PubMed 18819799 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.25 7.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL483397 1 7.02
CHEMBL485555 1 6.90
CHEMBL485564 1 6.85
CHEMBL519698 1 6.63
CHEMBL520312 1 6.26
CHEMBL483602 1 6.26
CHEMBL485233 1 6.26
CHEMBL485232 1 6.07
CHEMBL485565 1 5.75
CHEMBL483403 1 5.41
CHEMBL485402 1 5.31
CHEMBL485607 1 -
CHEMBL484941 1 -
CHEMBL484940 1 -
CHEMBL521468 1 -
CHEMBL485556 1 -
CHEMBL485399 1 -
CHEMBL484546 1 -
CHEMBL521484 1 -
CHEMBL485390 1 -
CHEMBL483181 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL483397 IC50 = 95.0 nM 7.02
CHEMBL485555 IC50 = 125.0 nM 6.90
CHEMBL485564 IC50 = 140.0 nM 6.85
CHEMBL519698 IC50 = 235.0 nM 6.63
CHEMBL520312 IC50 = 550.0 nM 6.26
CHEMBL483602 IC50 = 550.0 nM 6.26
CHEMBL485233 IC50 = 550.0 nM 6.26
CHEMBL485232 IC50 = 850.0 nM 6.07
CHEMBL485565 IC50 = 1800.0 nM 5.75
CHEMBL483403 IC50 = 3900.0 nM 5.41
CHEMBL485402 IC50 = 4900.0 nM 5.31
CHEMBL485607 IC50 > 10000.0 nM -
CHEMBL484941 IC50 - -
CHEMBL484940 IC50 > 10000.0 nM -
CHEMBL521468 IC50 > 10000.0 nM -
CHEMBL485556 IC50 > 10000.0 nM -
CHEMBL485399 IC50 - -
CHEMBL484546 IC50 - -
CHEMBL521484 IC50 - -
CHEMBL485390 IC50 - -
CHEMBL483181 IC50 > 10000.0 nM -