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Assay Detail

CHEMBL4478502

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

Binding
Binding affinity to human PIM1 (15 to 313 residues) expressed in bacterial system by KINOMEScan 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

Serine/threonine-protein kinase pim-1 (CHEMBL2147)
Type SINGLE PROTEIN
Organism Homo sapiens

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
Kd 1 8.89 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3979678 1 8.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3979678 Kd = 1.3 nM 8.89