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Compound Detail

CHEMBL132904

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CCOC(=O)c1cnc2oc3ccc(O)cc3c2c1-c1ccccc1

Basic Information

ChEMBL ID CHEMBL132904
Phase Preclinical
Structure Type MOL
InChI Key ZIAVUCXRGWKBBY-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

333.3
MW (Da)
4.53
ALogP
5
HBA
1
HBD
72.6
PSA (Ų)
0.56
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H15NO4
MW 333.34
Aromatic Rings 4
Heavy Atoms 25
NP-Likeness -0.14

Activity Summary

IC50 4 meas. best 5.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
CDK2/Cyclin A2
CHEMBL3038469
IC50 5.15 5.15 7100.0 1
Cyclin-dependent kinase 2/cyclin E1
CHEMBL1907605
IC50 4.84 4.84 14300.0 1
Cyclin-dependent kinase 1/cyclin B
CHEMBL2094127
IC50 4.54 4.54 28800.0 1
Unchecked
CHEMBL612545
IC50 4.54 4.54 28800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18077363 10.1073/pnas.0708800104 Unchecked 4
18077363 10.1073/pnas.0708800104 Serine/threonine-protein kinase 26 2
18077363 10.1073/pnas.0708800104 Ribosomal protein S6 kinase alpha-3 2
12593668 10.1021/jm021090g ATP-dependent translocase ABCB1 2
12593668 10.1021/jm021090g Cyclin-dependent kinase 5/CDK5 activator 1 2
18077363 10.1073/pnas.0708800104 Calcium/calmodulin-dependent protein kinase type 1D 1
12593668 10.1021/jm021090g Cyclin-dependent kinase 1/cyclin B 1
18077363 10.1073/pnas.0708800104 Calcium/calmodulin-dependent protein kinase type IV 1
18077363 10.1073/pnas.0708800104 Calcium/calmodulin-dependent protein kinase type II subunit gamma 1
30234987 10.1021/acs.jmedchem.8b00049 HCT-116 1
18077363 10.1073/pnas.0708800104 Calcium/calmodulin-dependent protein kinase type II subunit beta 1
18077363 10.1073/pnas.0708800104 Calcium/calmodulin-dependent protein kinase type II subunit alpha 1
18077363 10.1073/pnas.0708800104 Calcium/calmodulin-dependent protein kinase type 1G 1
12593668 10.1021/jm021090g Tumor Cell line 1
18077363 10.1073/pnas.0708800104 5'-AMP-activated protein kinase catalytic subunit alpha-2 1
12593668 10.1021/jm021090g IGROV-1 1
11814809 10.1016/s0960-894x(01)00769-7 NCI/ADR-RES 1
11814809 10.1016/s0960-894x(01)00769-7 IGROV-1 1
11814809 10.1016/s0960-894x(01)00769-7 SNB-75 1
11814809 10.1016/s0960-894x(01)00769-7 KM12 1

Data from ChEMBL 36 via Core Engine