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Assay Detail

CHEMBL4236804

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

Binding
Inhibition of recombinant human full length His-tagged JNK2 expressed in baculovirus expression system by Z'-LYTE assay
1
Total Activities
1
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

Mitogen-activated protein kinase 9 (CHEMBL4179)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4- d]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate N2-(2-Ethoxy-4-(4-methyl-4 H-1,2,4-triazol-3-yl)phenyl)-6-methyl- N8-neopentylpyrido[3,4- d]pyrimidine-2,8-diamine (BOS172722).
Woodward HL, Innocenti P, Cheung KJ, Hayes A, Roberts J, Henley AT, Faisal A, Mak GW, Box G, Westwood IM, Cronin N, Carter M, Valenti M, De Haven Brandon A, O'Fee L, Saville H, Schmitt J, Burke R, Broccatelli F, van Montfort RLM, Raynaud FI, Eccles SA, Linardopoulos S, Blagg J, Hoelder S.
J Med Chem (2018) 61 : 8226 -8240
PubMed 30199249 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.12 7.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3924132 BOS-172722 1.0 1 7.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3924132 BOS-172722 IC50 = 76.0 nM 7.12