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Assay Detail

CHEMBL5516679

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

Binding
Inhibition of human VRK1 (3 to 364 residues) expressed in Escherichia coli BL21 (DE3)-R3 cells assessed as inhibition constant using human histone H3 peptide as substrate preincubated for 30 mins followed by substrate and ATP addition incubated for 60 mins by Cheng-Prusoff equation based TR-FRET assay
ChEMBL ↗
42
Total Activities
42
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 VRK1 (CHEMBL1293199) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel Dihydropteridinone Derivatives As Potent Inhibitors of the Understudied Human Kinases Vaccinia-Related Kinase 1 and Casein Kinase 1δ/ε.
de Souza Gama FH, Dutra LA, Hawgood M, Dos Reis CV, Serafim RAM, Ferreira MA, Teodoro BVM, Takarada JE, Santiago AS, Balourdas DI, Nilsson AS, Urien B, Almeida VM, Gileadi C, Ramos PZ, Salmazo A, Vasconcelos SNS, Cunha MR, Mueller S, Knapp S, Massirer KB, Elkins JM, Gileadi O, Mascarello A, Lemmens BBLG, Guimarães CRW, Azevedo H, Couñago RM.
J Med Chem (2024) 67 : 8609 -8629
PubMed 38780468 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 42 7.23 7.87

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5561272 — — 1 7.87
CHEMBL5557609 — — 1 7.75
CHEMBL5557379 — — 1 7.66
CHEMBL5564158 — — 1 7.64
CHEMBL5557387 — — 1 7.58
CHEMBL5566532 — — 1 7.58
CHEMBL5557355 — — 1 7.58
CHEMBL5557932 — — 1 7.51
CHEMBL5523509 — — 1 7.50
CHEMBL5532198 — — 1 7.50
CHEMBL5542657 — — 1 7.47
CHEMBL5559444 — — 1 7.45
CHEMBL5555299 — — 1 7.43
CHEMBL5558036 — — 1 7.43
CHEMBL5557062 — — 1 7.42
CHEMBL5542121 — — 1 7.30
CHEMBL573107 — — 1 7.25
CHEMBL5557286 — — 1 7.21
CHEMBL5564373 — — 1 7.18
CHEMBL5549880 — — 1 7.18
CHEMBL5562568 — — 1 7.14
CHEMBL5557942 — — 1 7.09
CHEMBL5542207 — — 1 7.06
CHEMBL5568610 — — 1 7.03
CHEMBL5558898 — — 1 7.03
CHEMBL3604889 — — 1 7.00
CHEMBL5565622 — — 1 6.98
CHEMBL5555994 — — 1 6.92
CHEMBL5532547 — — 1 6.90
CHEMBL5563756 — — 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5561272 — Ki = 13.6 nM 7.87
CHEMBL5557609 — Ki = 17.9 nM 7.75
CHEMBL5557379 — Ki = 21.8 nM 7.66
CHEMBL5564158 — Ki = 23.1 nM 7.64
CHEMBL5557387 — Ki = 26.1 nM 7.58
CHEMBL5566532 — Ki = 26.5 nM 7.58
CHEMBL5557355 — Ki = 26.1 nM 7.58
CHEMBL5557932 — Ki = 31.0 nM 7.51
CHEMBL5523509 — Ki = 31.7 nM 7.50
CHEMBL5532198 — Ki = 31.5 nM 7.50
CHEMBL5542657 — Ki = 33.8 nM 7.47
CHEMBL5559444 — Ki = 35.2 nM 7.45
CHEMBL5555299 — Ki = 36.7 nM 7.43
CHEMBL5558036 — Ki = 36.9 nM 7.43
CHEMBL5557062 — Ki = 37.9 nM 7.42
CHEMBL5542121 — Ki = 50.0 nM 7.30
CHEMBL573107 — Ki = 56.1 nM 7.25
CHEMBL5557286 — Ki = 62.2 nM 7.21
CHEMBL5564373 — Ki = 66.2 nM 7.18
CHEMBL5549880 — Ki = 66.5 nM 7.18
CHEMBL5562568 — Ki = 72.6 nM 7.14
CHEMBL5557942 — Ki = 80.9 nM 7.09
CHEMBL5542207 — Ki = 87.3 nM 7.06
CHEMBL5568610 — Ki = 94.0 nM 7.03
CHEMBL5558898 — Ki = 94.2 nM 7.03
CHEMBL3604889 — Ki = 100.7 nM 7.00
CHEMBL5565622 — Ki = 104.7 nM 6.98
CHEMBL5555994 — Ki = 121.1 nM 6.92
CHEMBL5532547 — Ki = 126.8 nM 6.90
CHEMBL5563756 — Ki = 128.2 nM 6.89
CHEMBL5561979 — Ki = 128.8 nM 6.89
CHEMBL5561159 — Ki = 134.6 nM 6.87
CHEMBL5559784 — Ki = 181.6 nM 6.74
CHEMBL5560770 — Ki = 183.2 nM 6.74
CHEMBL5562037 — Ki = 194.1 nM 6.71
CHEMBL5557685 — Ki = 213.8 nM 6.67
CHEMBL5556356 — Ki - — -
CHEMBL5557764 — Ki - — -
CHEMBL5542808 — Ki - — -
CHEMBL5563167 — Ki - — -
CHEMBL5567144 — Ki - — -
CHEMBL5565297 — Ki - — -