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Assay Detail

CHEMBL4035520

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Binding
Binding affinity to CK2alpha (unknown origin) by ITC
11
Total Activities
11
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

Casein kinase II subunit alpha (CHEMBL3629)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A fragment-based approach leading to the discovery of a novel binding site and the selective CK2 inhibitor CAM4066.
De Fusco C, Brear P, Iegre J, Georgiou KH, Sore HF, Hyvönen M, Spring DR.
Bioorg Med Chem (2017) 25 : 3471 -3482
PubMed 28495381 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 11 4.18 6.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4070389 1 6.50
CHEMBL4086439 1 5.79
CHEMBL1161012 1 4.24
CHEMBL4089903 1 3.57
CHEMBL4105345 1 3.52
CHEMBL4082041 1 3.30
CHEMBL4061844 1 3.28
CHEMBL4100054 1 3.20
CHEMBL307782 3-AMINOBENZOIC ACID 1 -
CHEMBL4088836 1 -
CHEMBL4104331 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4070389 Kd = 320.0 nM 6.50
CHEMBL4086439 Kd = 1640.0 nM 5.79
CHEMBL1161012 Kd = 58000.0 nM 4.24
CHEMBL4089903 Kd = 270000.0 nM 3.57
CHEMBL4105345 Kd = 300000.0 nM 3.52
CHEMBL4082041 Kd = 500000.0 nM 3.30
CHEMBL4061844 Kd = 520000.0 nM 3.28
CHEMBL4100054 Kd = 629000.0 nM 3.20
CHEMBL307782 3-AMINOBENZOIC ACID Kd > 500000.0 nM -
CHEMBL4088836 Kd = 250000.0 nM -
CHEMBL4104331 Kd = 250000.0 nM -