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Assay Detail

CHEMBL830066

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

Binding
In vitro inhibition of SR protein kinase 1 by compound dissolved in 100% DMSO using 5''-[gamma-33P]-triphosphate
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Ribosomal protein S6 kinase beta-2 (CHEMBL3111)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of selective SRPK-1 inhibitors: novel tricyclic quinoxaline derivatives.
Székelyhidi Z, Pató J, Wáczek F, Bánhegyi P, Hegymegi-Barakonyi B, Erös D, Mészáros G, Hollósy F, Hafenbradl D, Obert S, Klebl B, Kéri G, Orfi L.
Bioorg Med Chem Lett (2005) 15 : 3241 -3246
PubMed 15925511 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 5.57 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL426445 1 7.40
CHEMBL192909 1 6.19
CHEMBL190057 1 6.09
CHEMBL366201 1 6.06
CHEMBL193232 1 6.02
CHEMBL193172 1 5.94
CHEMBL193162 1 5.89
CHEMBL364499 1 5.87
CHEMBL190143 1 5.21
CHEMBL190039 1 5.02
CHEMBL366185 1 5.00
CHEMBL192974 1 4.93
CHEMBL373367 1 4.79
CHEMBL192489 1 4.63
CHEMBL189940 1 4.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL426445 IC50 = 40.0 nM 7.40
CHEMBL192909 IC50 = 640.0 nM 6.19
CHEMBL190057 IC50 = 820.0 nM 6.09
CHEMBL366201 IC50 = 870.0 nM 6.06
CHEMBL193232 IC50 = 950.0 nM 6.02
CHEMBL193172 IC50 = 1140.0 nM 5.94
CHEMBL193162 IC50 = 1280.0 nM 5.89
CHEMBL364499 IC50 = 1360.0 nM 5.87
CHEMBL190143 IC50 = 6130.0 nM 5.21
CHEMBL190039 IC50 = 9610.0 nM 5.02
CHEMBL366185 IC50 = 10000.0 nM 5.00
CHEMBL192974 IC50 = 11750.0 nM 4.93
CHEMBL373367 IC50 = 16310.0 nM 4.79
CHEMBL192489 IC50 = 23360.0 nM 4.63
CHEMBL189940 IC50 = 28490.0 nM 4.54