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Assay Detail

CHEMBL4052121

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

Binding
Inhibition of PIM3 (unknown origin) using 5FAM-ARKRRRHPSGPPTA as substrate after 90 mins in presence of ATP by caliper microfluidic mobility shift assay
17
Total Activities
17
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-3 (CHEMBL5407)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 5-Azaindazole (GNE-955) as a Potent Pan-Pim Inhibitor with Optimized Bioavailability.
Wang X, Kolesnikov A, Tay S, Chan G, Chao Q, Do S, Drummond J, Ebens AJ, Liu N, Ly J, Harstad E, Hu H, Moffat J, Munugalavadla V, Murray J, Slaga D, Tsui V, Volgraf M, Wallweber H, Chang JH.
J Med Chem (2017) 60 : 4458 -4473
PubMed 28445037 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 9.45 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3634758 1 10.70
CHEMBL3960554 1 10.70
CHEMBL4076913 1 10.70
CHEMBL3956349 1 10.70
CHEMBL4091687 1 10.52
CHEMBL3978766 1 10.40
CHEMBL3956461 1 10.00
CHEMBL4097308 1 9.70
CHEMBL3915064 1 9.70
CHEMBL4089586 1 9.40
CHEMBL4061456 1 9.40
CHEMBL4070117 1 9.10
CHEMBL4081716 1 9.00
CHEMBL4088342 1 7.64
CHEMBL4060101 1 6.92
CHEMBL4099731 1 6.57
CHEMBL3914639 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3634758 Ki = 0.02 nM 10.70
CHEMBL3960554 Ki = 0.02 nM 10.70
CHEMBL4076913 Ki = 0.02 nM 10.70
CHEMBL3956349 Ki = 0.02 nM 10.70
CHEMBL4091687 Ki = 0.03 nM 10.52
CHEMBL3978766 Ki = 0.04 nM 10.40
CHEMBL3956461 Ki = 0.1 nM 10.00
CHEMBL4097308 Ki = 0.2 nM 9.70
CHEMBL3915064 Ki = 0.2 nM 9.70
CHEMBL4089586 Ki = 0.4 nM 9.40
CHEMBL4061456 Ki = 0.4 nM 9.40
CHEMBL4070117 Ki = 0.8 nM 9.10
CHEMBL4081716 Ki = 1.0 nM 9.00
CHEMBL4088342 Ki = 23.0 nM 7.64
CHEMBL4060101 Ki = 120.0 nM 6.92
CHEMBL4099731 Ki = 270.0 nM 6.57
CHEMBL3914639 Ki = 0.008 nM -