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

CHEMBL4359940

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

Binding
Inhibition of human recombinant full length His6-tagged IRAK4 expressed in baculovirus expression system using H-KKARFSRFAGSSPSQSSMVAR as substrate incubated for 90 mins by fluorescence polarisation assay
36
Total Activities
36
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

Development of Potent and Selective Pyrazolopyrimidine IRAK4 Inhibitors.
Bryan MC, Drobnick J, Gobbi A, Kolesnikov A, Chen Y, Rajapaksa N, Ndubaku C, Feng J, Chang W, Francis R, Yu C, Choo EF, DeMent K, Ran Y, An L, Emson C, Huang Z, Sujatha-Bhaskar S, Brightbill H, DiPasquale A, Maher J, Wai J, McKenzie BS, Lupardus PJ, Zarrin AA, Kiefer JR.
J Med Chem (2019) 62 : 6223 -6240
PubMed 31082230 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 36 8.19 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4474636 1 9.30
CHEMBL4464832 1 9.30
CHEMBL4568867 1 9.10
CHEMBL4520118 1 8.96
CHEMBL4515682 1 8.92
CHEMBL4467170 1 8.82
CHEMBL4460055 1 8.77
CHEMBL4453861 1 8.77
CHEMBL4483477 1 8.74
CHEMBL3950656 1 8.70
CHEMBL4483551 1 8.68
CHEMBL4461516 1 8.49
CHEMBL4466092 1 8.49
CHEMBL4438027 1 8.46
CHEMBL4466517 1 8.29
CHEMBL4473269 1 8.28
CHEMBL4531013 1 8.24
CHEMBL4456286 1 8.21
CHEMBL4518559 1 8.19
CHEMBL4584820 1 8.18
CHEMBL4554579 1 8.17
CHEMBL4576141 1 8.14
CHEMBL4524886 1 8.13
CHEMBL4452936 1 8.00
CHEMBL4459509 1 7.92
CHEMBL4569547 1 7.89
CHEMBL4439253 1 7.82
CHEMBL4551768 1 7.58
CHEMBL4462969 1 7.51
CHEMBL4474664 1 7.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4474636 Ki = 0.5 nM 9.30
CHEMBL4464832 Ki = 0.5 nM 9.30
CHEMBL4568867 Ki = 0.8 nM 9.10
CHEMBL4520118 Ki = 1.1 nM 8.96
CHEMBL4515682 Ki = 1.2 nM 8.92
CHEMBL4467170 Ki = 1.5 nM 8.82
CHEMBL4460055 Ki = 1.7 nM 8.77
CHEMBL4453861 Ki = 1.7 nM 8.77
CHEMBL4483477 Ki = 1.8 nM 8.74
CHEMBL3950656 Ki = 2.0 nM 8.70
CHEMBL4483551 Ki = 2.1 nM 8.68
CHEMBL4461516 Ki = 3.2 nM 8.49
CHEMBL4466092 Ki = 3.2 nM 8.49
CHEMBL4438027 Ki = 3.5 nM 8.46
CHEMBL4466517 Ki = 5.1 nM 8.29
CHEMBL4473269 Ki = 5.3 nM 8.28
CHEMBL4531013 Ki = 5.8 nM 8.24
CHEMBL4456286 Ki = 6.1 nM 8.21
CHEMBL4518559 Ki = 6.5 nM 8.19
CHEMBL4584820 Ki = 6.6 nM 8.18
CHEMBL4554579 Ki = 6.7 nM 8.17
CHEMBL4576141 Ki = 7.3 nM 8.14
CHEMBL4524886 Ki = 7.4 nM 8.13
CHEMBL4452936 Ki = 10.0 nM 8.00
CHEMBL4459509 Ki = 12.0 nM 7.92
CHEMBL4569547 Ki = 13.0 nM 7.89
CHEMBL4439253 Ki = 15.0 nM 7.82
CHEMBL4551768 Ki = 26.0 nM 7.58
CHEMBL4462969 Ki = 31.0 nM 7.51
CHEMBL4474664 Ki = 34.0 nM 7.47
CHEMBL4550566 Ki = 35.0 nM 7.46
CHEMBL3952937 Ki = 52.0 nM 7.28
CHEMBL4436128 Ki = 95.0 nM 7.02
CHEMBL4544284 Ki = 170.0 nM 6.77
CHEMBL4460458 Ki = 290.0 nM 6.54
CHEMBL4463353 Ki > 8400.0 nM -