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Assay Detail

CHEMBL923138

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Binding
Inhibition of Btk
4
Total Activities
4
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 BTK (CHEMBL5251)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

N-4-Pyrimidinyl-1H-indazol-4-amine inhibitors of Lck: indazoles as phenol isosteres with improved pharmacokinetics.
Bamborough P, Angell RM, Bhamra I, Brown D, Bull J, Christopher JA, Cooper AW, Fazal LH, Giordano I, Hind L, Patel VK, Ranshaw LE, Sims MJ, Skone PA, Smith KJ, Vickerstaff E, Washington M.
Bioorg Med Chem Lett (2007) 17 : 4363 -4368
PubMed 17600705 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.41 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL249097 1 8.05
CHEMBL248676 1 7.16
CHEMBL398422 1 7.01
CHEMBL249317 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL249097 IC50 = 9.0 nM 8.05
CHEMBL248676 IC50 = 69.0 nM 7.16
CHEMBL398422 IC50 = 97.0 nM 7.01
CHEMBL249317 IC50 - -