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Assay Detail

CHEMBL5550419

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

Binding
Inhibition of recombinant human Haspin kinase domain (470 to 798 residues) expressed in bacteria using histone H3 (1 to 21) peptide as substrate incubated for 30 mins in presence of ATP by ADP-Glo kinase assay
16
Total Activities
16
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 haspin (CHEMBL1075163)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of 1H-pyrrolo[3,2-g]isoquinolines.
Defois M, Josselin B, Brindeau P, Krämer A, Knapp S, Anizon F, Giraud F, Ruchaud S, Moreau P.
Bioorg Med Chem (2024) 100 : 117619 -117619
PubMed 38320389 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.95 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5178368 1 8.70
CHEMBL5181620 1 7.30
CHEMBL5594716 1 7.21
CHEMBL5569099 1 7.12
CHEMBL5570490 1 7.12
CHEMBL5563473 1 6.94
CHEMBL5574139 1 6.91
CHEMBL5562930 1 6.89
CHEMBL5592689 1 6.82
CHEMBL5571626 1 6.80
CHEMBL5564481 1 6.80
CHEMBL5574327 1 6.61
CHEMBL5563580 1 6.60
CHEMBL5569713 1 6.32
CHEMBL5574287 1 6.09
CHEMBL5595643 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5178368 IC50 = 2.0 nM 8.70
CHEMBL5181620 IC50 = 50.0 nM 7.30
CHEMBL5594716 IC50 = 62.0 nM 7.21
CHEMBL5569099 IC50 = 75.0 nM 7.12
CHEMBL5570490 IC50 = 76.0 nM 7.12
CHEMBL5563473 IC50 = 114.0 nM 6.94
CHEMBL5574139 IC50 = 122.0 nM 6.91
CHEMBL5562930 IC50 = 130.0 nM 6.89
CHEMBL5592689 IC50 = 150.0 nM 6.82
CHEMBL5571626 IC50 = 158.0 nM 6.80
CHEMBL5564481 IC50 = 157.0 nM 6.80
CHEMBL5574327 IC50 = 243.0 nM 6.61
CHEMBL5563580 IC50 = 249.0 nM 6.60
CHEMBL5569713 IC50 = 482.0 nM 6.32
CHEMBL5574287 IC50 = 819.0 nM 6.09
CHEMBL5595643 IC50 ~ 1000.0 nM -