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Assay Detail

CHEMBL2387969

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

Binding
Inhibition of PIM2 (unknown origin) using FAM-pimtide as substrate after 90 mins by spectrophotometry in presence of ATP
18
Total Activities
18
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-2 (CHEMBL4523)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of novel pyrazolo[1,5-a]pyrimidines as potent pan-Pim inhibitors by structure- and property-based drug design.
Wang X, Magnuson S, Pastor R, Fan E, Hu H, Tsui V, Deng W, Murray J, Steffek M, Wallweber H, Moffat J, Drummond J, Chan G, Harstad E, Ebens AJ.
Bioorg Med Chem Lett (2013) 23 : 3149 -3153
PubMed 23623490 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 8.79 10.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2387464 1 10.49
CHEMBL2387465 1 10.43
CHEMBL2387471 1 10.12
CHEMBL2387463 1 10.03
CHEMBL2387474 1 9.77
CHEMBL2387473 1 9.28
CHEMBL2387475 1 9.19
CHEMBL2387472 1 8.89
CHEMBL2387479 1 8.70
CHEMBL2387469 1 8.66
CHEMBL2387468 1 8.55
CHEMBL2387462 1 8.31
CHEMBL2387478 1 8.23
CHEMBL2387470 1 8.11
CHEMBL2387476 1 7.75
CHEMBL2387477 1 7.68
CHEMBL2387467 1 7.51
CHEMBL2387466 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2387464 Ki = 0.032 nM 10.49
CHEMBL2387465 Ki = 0.037 nM 10.43
CHEMBL2387471 Ki = 0.076 nM 10.12
CHEMBL2387463 Ki = 0.094 nM 10.03
CHEMBL2387474 Ki = 0.17 nM 9.77
CHEMBL2387473 Ki = 0.52 nM 9.28
CHEMBL2387475 Ki = 0.65 nM 9.19
CHEMBL2387472 Ki = 1.3 nM 8.89
CHEMBL2387479 Ki = 2.0 nM 8.70
CHEMBL2387469 Ki = 2.2 nM 8.66
CHEMBL2387468 Ki = 2.8 nM 8.55
CHEMBL2387462 Ki = 4.9 nM 8.31
CHEMBL2387478 Ki = 5.9 nM 8.23
CHEMBL2387470 Ki = 7.8 nM 8.11
CHEMBL2387476 Ki = 18.0 nM 7.75
CHEMBL2387477 Ki = 21.0 nM 7.68
CHEMBL2387467 Ki = 31.0 nM 7.51
CHEMBL2387466 Ki = 250.0 nM 6.60