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Assay Detail

CHEMBL1685407

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

Binding
Inhibition of Pim1 after 1 hr using biotinylated AL1peptide as substrate
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Scaffold oriented synthesis. Part 3: design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing [2+3] cycloadditions.
Akritopoulou-Zanze I, Wakefield BD, Gasiecki A, Kalvin D, Johnson EF, Kovar P, Djuric SW.
Bioorg Med Chem Lett (2011) 21 : 1476 -1479
PubMed 21282054 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 5.06 6.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1682345 1 6.04
CHEMBL1682344 1 5.65
CHEMBL1681795 1 5.43
CHEMBL1682347 1 5.38
CHEMBL1682358 1 5.29
CHEMBL1682335 1 5.08
CHEMBL1682350 1 4.99
CHEMBL1682351 1 4.92
CHEMBL1682354 1 4.69
CHEMBL1682355 1 4.44
CHEMBL1682349 1 4.42
CHEMBL1682356 1 4.38
CHEMBL1682336 1 -
CHEMBL1682337 1 -
CHEMBL1682338 1 -
CHEMBL1682339 1 -
CHEMBL1682340 1 -
CHEMBL1682341 1 -
CHEMBL1682342 1 -
CHEMBL1682343 1 -
CHEMBL1682346 1 -
CHEMBL1682352 1 -
CHEMBL1682360 1 -
CHEMBL1682359 1 -
CHEMBL1682357 1 -
CHEMBL1682353 1 -
CHEMBL1682348 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1682345 Ki = 923.0 nM 6.04
CHEMBL1682344 Ki = 2219.0 nM 5.65
CHEMBL1681795 Ki = 3685.0 nM 5.43
CHEMBL1682347 Ki = 4153.0 nM 5.38
CHEMBL1682358 Ki = 5155.0 nM 5.29
CHEMBL1682335 Ki = 8359.0 nM 5.08
CHEMBL1682350 Ki = 10153.0 nM 4.99
CHEMBL1682351 Ki = 12000.0 nM 4.92
CHEMBL1682354 Ki = 20307.0 nM 4.69
CHEMBL1682355 Ki = 36000.0 nM 4.44
CHEMBL1682349 Ki = 37846.0 nM 4.42
CHEMBL1682356 Ki = 41538.0 nM 4.38
CHEMBL1682336 Ki > 8570.0 nM -
CHEMBL1682337 Ki > 8570.0 nM -
CHEMBL1682338 Ki > 8570.0 nM -
CHEMBL1682339 Ki > 8570.0 nM -
CHEMBL1682340 Ki > 8570.0 nM -
CHEMBL1682341 Ki > 8570.0 nM -
CHEMBL1682342 Ki > 8570.0 nM -
CHEMBL1682343 Ki > 8570.0 nM -
CHEMBL1682346 Ki > 8570.0 nM -
CHEMBL1682352 Ki = 165230.0 nM -
CHEMBL1682360 Ki > 8570.0 nM -
CHEMBL1682359 Ki > 8570.0 nM -
CHEMBL1682357 Ki > 8570.0 nM -
CHEMBL1682353 Ki - -
CHEMBL1682348 Ki - -