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

CHEMBL4478537

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

Functional
In vivo inhibition of pan Pim in SCID-bg mouse xenografted with human KMS-12-BM cells assessed as plasma concentration required for reduction of BAD peptide phosphorylation at Serine 112 residue at 10 to 100 mg/kg, po qd measured after 1 to 24 hrs post dose
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Confidence 1 — Organism
Curated By Autocuration

Target

Mus musculus (CHEMBL375)
Type ORGANISM
Organism Mus musculus

Publication

Discovery and Optimization of Quinazolinone-pyrrolopyrrolones as Potent and Orally Bioavailable Pan-Pim Kinase Inhibitors.
Pettus LH, Andrews KL, Booker SK, Chen J, Cee VJ, Chavez F, Chen Y, Eastwood H, Guerrero N, Herberich B, Hickman D, Lanman BA, Laszlo J, Lee MR, Lipford JR, Mattson B, Mohr C, Nguyen Y, Norman MH, Powers D, Reed AB, Rex K, Sastri C, Tamayo N, Wang P, Winston JT, Wu B, Wu T, Wurz RP, Xu Y, Zhou Y, Tasker AS, Wang HL.
J Med Chem (2016) 59 : 6407 -6430
PubMed 27285051 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 6.59 6.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3979678 1 6.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3979678 EC50 = 254.0 nM 6.59