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Assay Detail

CHEMBL4345130

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

Binding
Inhibition of recombinant full-length N-terminal His6-tagged human IRAK4 expressed in baculovirus expression system using H-KKARFSRFAGSSPSQSSMVAR peptide as substrate after 90 mins by fluorescence polarisation assay
21
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Interleukin-1 receptor-associated kinase 4 (CHEMBL3778)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Potent Benzolactam IRAK4 Inhibitors with Robust in Vivo Activity.
Rajapaksa NS, Gobbi A, Drobnick J, Do S, Kolesnikov A, Liang J, Chen Y, Sujatha-Bhaskar S, Huang Z, Brightbill H, Francis R, Yu C, Choo EF, DeMent K, Ran Y, An L, Emson C, Maher J, Wai J, McKenzie BS, Lupardus PJ, Zarrin AA, Kiefer JR, Bryan MC.
ACS Med Chem Lett (2020) 11 : 327 -333
PubMed 32184965 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.96 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4475494 1 8.85
CHEMBL4556091 1 8.72
CHEMBL4466981 1 8.72
CHEMBL4472406 1 8.66
CHEMBL4545898 1 8.59
CHEMBL4568894 1 8.47
CHEMBL4445098 1 8.46
CHEMBL4452765 1 8.43
CHEMBL4566431 1 8.43
CHEMBL4473269 1 8.30
CHEMBL4439292 2 8.21
CHEMBL4536154 1 8.11
CHEMBL4444608 1 7.85
CHEMBL4537890 1 7.72
CHEMBL4464216 2 7.66
CHEMBL4468790 1 7.58
CHEMBL4557715 1 7.52
CHEMBL4592237 1 7.10
CHEMBL4518564 1 6.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4475494 Ki = 1.4 nM 8.85
CHEMBL4556091 Ki = 1.9 nM 8.72
CHEMBL4466981 Ki = 1.9 nM 8.72
CHEMBL4472406 Ki = 2.2 nM 8.66
CHEMBL4545898 Ki = 2.6 nM 8.59
CHEMBL4568894 Ki = 3.4 nM 8.47
CHEMBL4445098 Ki = 3.5 nM 8.46
CHEMBL4566431 Ki = 3.7 nM 8.43
CHEMBL4452765 Ki = 3.7 nM 8.43
CHEMBL4473269 Ki = 5.0 nM 8.30
CHEMBL4439292 Ki = 6.1 nM 8.21
CHEMBL4536154 Ki = 7.8 nM 8.11
CHEMBL4444608 Ki = 14.0 nM 7.85
CHEMBL4537890 Ki = 19.0 nM 7.72
CHEMBL4464216 Ki = 22.0 nM 7.66
CHEMBL4468790 Ki = 26.0 nM 7.58
CHEMBL4557715 Ki = 30.0 nM 7.52
CHEMBL4592237 Ki = 80.0 nM 7.10
CHEMBL4439292 Ki = 160.0 nM 6.80
CHEMBL4518564 Ki = 210.0 nM 6.68
CHEMBL4464216 Ki = 490.0 nM 6.31