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Compound Detail

CHEMBL5191835

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O=C(O)Cc1ccc(O)cc1Oc1ccccc1Cl

Basic Information

ChEMBL ID CHEMBL5191835
Phase Preclinical
Structure Type MOL
InChI Key AMHXRNDEHCSZKC-UHFFFAOYSA-N
2
Targets
12
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

278.7
MW (Da)
3.47
ALogP
3
HBA
2
HBD
66.8
PSA (Ų)
0.90
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H11ClO4
MW 278.69
Aromatic Rings 2
Heavy Atoms 19
NP-Likeness -0.04

Activity Summary

Kd 6 meas. best 6.66
Ki 6 meas. best 7.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Calcium/calmodulin-dependent protein kinase type II subunit alpha
CHEMBL2359
Ki 7.6 7.4375 25.1 4
Calcium/calmodulin-dependent protein kinase type II subunit alpha
CHEMBL4147
Kd 6.66 6.66 219.0 6
Calcium/calmodulin-dependent protein kinase type II subunit alpha
CHEMBL4147
Ki 6.3 6.3 500.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Calcium/calmodulin-dependent protein kinase type II subunit alpha Ki = 25.12 nM 7.6 Displacement of [3H]NCS-382 from CaMK2alpha in rat brain cerebral cortex membran... 35500061
Calcium/calmodulin-dependent protein kinase type II subunit alpha Ki = 27.0 nM 7.57 Displacement of [3H]NCS-382 from CaMK2alpha in rat brain cerebral cortex membran... 35500061
Calcium/calmodulin-dependent protein kinase type II subunit alpha Ki = 50.12 nM 7.3 Displacement of [3H]HOCPCA from CaMK2alpha in rat brain cerebral cortex membrane... 35500061
Calcium/calmodulin-dependent protein kinase type II subunit alpha Ki = 53.0 nM 7.28 Displacement of [3H]HOCPCA from CaMK2alpha in rat brain cerebral cortex membrane... 35500061
Calcium/calmodulin-dependent protein kinase type II subunit alpha Kd = 219.0 nM 6.66 Binding affinity to recombinant human CaMK2alpha Thr354Asn mutant expressed in E... 35500061
Calcium/calmodulin-dependent protein kinase type II subunit alpha Kd = 219.0 nM 6.66 Binding affinity to recombinant human CaMK2alpha Glu355Gln mutant expressed in E... 35500061
Calcium/calmodulin-dependent protein kinase type II subunit alpha Kd = 219.0 nM 6.66 Binding affinity to recombinant human CaMK2alpha Thr412Asn mutant expressed in E... 35500061
Calcium/calmodulin-dependent protein kinase type II subunit alpha Kd = 219.0 nM 6.66 Binding affinity to recombinant human CaMK2alpha Ile414Met mutant expressed in E... 35500061
Calcium/calmodulin-dependent protein kinase type II subunit alpha Kd = 219.0 nM 6.66 Binding affinity to recombinant human CaMK2alpha Ile464His mutant expressed in E... 35500061
Calcium/calmodulin-dependent protein kinase type II subunit alpha Kd = 219.0 nM 6.66 Binding affinity to recombinant human CaMK2alpha Phe467Met mutant expressed in E... 35500061
Calcium/calmodulin-dependent protein kinase type II subunit alpha Ki = 500.0 nM 6.3 Displacement of [3H]HOCPCA from recombinant full length CaMK2alpha (unknown orig... 35500061
Calcium/calmodulin-dependent protein kinase type II subunit alpha Ki = 501.19 nM 6.3 Displacement of [3H]HOCPCA from recombinant full length CaMK2alpha (unknown orig... 35500061

Literature References

PubMed DOI Target Context # Activities
35500061 10.1021/acs.jmedchem.1c02177 Calcium/calmodulin-dependent protein kinase type II subunit alpha 13
35500061 10.1021/acs.jmedchem.1c02177 ADMET 4
35500061 10.1021/acs.jmedchem.1c02177 No relevant target 3

Data from ChEMBL 36 via Core Engine