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Assay Detail

CHEMBL1059320

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Binding
Inhibition of human PIM3 by scintillation counting
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Serine/threonine-protein kinase pim-3 (CHEMBL5407)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 3H-benzo[4,5]thieno[3,2-d]pyrimidin-4-ones as potent, highly selective, and orally bioavailable inhibitors of the human protooncogene proviral insertion site in moloney murine leukemia virus (PIM) kinases.
Tao ZF, Hasvold LA, Leverson JD, Han EK, Guan R, Johnson EF, Stoll VS, Stewart KD, Stamper G, Soni N, Bouska JJ, Luo Y, Sowin TJ, Lin NH, Giranda VS, Rosenberg SH, Penning TD.
J Med Chem (2009) 52 : 6621 -6636
PubMed 19842661 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 8.94 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL576387 1 9.70
CHEMBL583273 1 9.52
CHEMBL572781 1 9.52
CHEMBL583187 1 9.40
CHEMBL585182 1 9.30
CHEMBL582844 1 9.15
CHEMBL572550 1 9.05
CHEMBL573702 1 9.00
CHEMBL584161 1 8.40
CHEMBL583144 1 7.96
CHEMBL573929 1 7.37
CHEMBL573012 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL576387 Ki = 0.2 nM 9.70
CHEMBL583273 Ki = 0.3 nM 9.52
CHEMBL572781 Ki = 0.3 nM 9.52
CHEMBL583187 Ki = 0.4 nM 9.40
CHEMBL585182 Ki = 0.5 nM 9.30
CHEMBL582844 Ki = 0.7 nM 9.15
CHEMBL572550 Ki = 0.9 nM 9.05
CHEMBL573702 Ki = 1.0 nM 9.00
CHEMBL584161 Ki = 4.0 nM 8.40
CHEMBL583144 Ki = 11.0 nM 7.96
CHEMBL573929 Ki = 43.0 nM 7.37
CHEMBL573012 Ki < 0.1 nM -