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Assay Detail

CHEMBL5034574

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

Binding
Inhibition of PIM1 (unknown origin) by ADP hunter plus assay
13
Total Activities
13
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

Fragment-Derived Selective Inhibitors of Dual-Specificity Kinases DYRK1A and DYRK1B.
Lee Walmsley D, Murray JB, Dokurno P, Massey AJ, Benwell K, Fiumana A, Foloppe N, Ray S, Smith J, Surgenor AE, Edmonds T, Demarles D, Burbridge M, Cruzalegui F, Kotschy A, Hubbard RE.
J Med Chem (2021) 64 : 8971 -8991
PubMed 34143631 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.67 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5091510 1 7.10
CHEMBL5090676 1 6.44
CHEMBL5085656 1 6.31
CHEMBL5081341 1 5.55
CHEMBL5082044 1 5.43
CHEMBL5092157 1 5.39
CHEMBL5083159 1 5.38
CHEMBL5092828 1 5.21
CHEMBL5092245 1 5.02
CHEMBL5076145 1 4.87
CHEMBL5083242 1 -
CHEMBL5090159 1 -
CHEMBL5081888 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5091510 IC50 = 79.0 nM 7.10
CHEMBL5090676 IC50 = 360.0 nM 6.44
CHEMBL5085656 IC50 = 489.0 nM 6.31
CHEMBL5081341 IC50 = 2800.0 nM 5.55
CHEMBL5082044 IC50 = 3700.0 nM 5.43
CHEMBL5092157 IC50 = 4100.0 nM 5.39
CHEMBL5083159 IC50 = 4200.0 nM 5.38
CHEMBL5092828 IC50 = 6200.0 nM 5.21
CHEMBL5092245 IC50 = 9600.0 nM 5.02
CHEMBL5076145 IC50 = 13600.0 nM 4.87
CHEMBL5083242 IC50 > 50000.0 nM -
CHEMBL5090159 IC50 > 50000.0 nM -
CHEMBL5081888 IC50 > 50000.0 nM -