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Compound Detail

CHEMBL5757213

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Cc1nc2c(F)cc(-c3nc(Nc4ccc5c(n4)CCN(CCCN(C)C)C5)ncc3F)cc2n1C1CC1

Basic Information

ChEMBL ID CHEMBL5757213
Phase Preclinical
Structure Type MOL
InChI Key GYDXFTMHNUETBY-UHFFFAOYSA-N
7
Targets
14
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

518.6
MW (Da)
4.86
ALogP
8
HBA
1
HBD
75.0
PSA (Ų)
0.36
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H32F2N8
MW 518.62
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -1.45

Activity Summary

IC50 14 meas. best 8.78

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 4
CHEMBL331
IC50 8.78 8.78 1.7 2
Cyclin-dependent kinase 6
CHEMBL2508
IC50 8.26 8.26 5.5 2
Cyclin-dependent kinase 7
CHEMBL3055
IC50 6.71 6.71 196.0 2
Cyclin-dependent kinase 9
CHEMBL3116
IC50 6.5 6.5 316.0 2
Cyclin-dependent kinase 5
CHEMBL4036
IC50 6.21 6.21 620.0 2
Cyclin-dependent kinase 2
CHEMBL301
IC50 5.83 5.83 1490.0 2
Cyclin-dependent kinase 1
CHEMBL308
IC50 5.44 5.44 3614.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 4 IC50 = 1.68 nM 8.78 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 4 IC50 = 1.68 nM 8.78 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 6 IC50 = 5.51 nM 8.26 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 6 IC50 = 5.51 nM 8.26 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 7 IC50 = 196.0 nM 6.71 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 7 IC50 = 196.0 nM 6.71 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 9 IC50 = 316.0 nM 6.5 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 9 IC50 = 316.0 nM 6.5 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 5 IC50 = 620.0 nM 6.21 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 5 IC50 = 620.0 nM 6.21 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 2 IC50 = 1490.0 nM 5.83 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 2 IC50 = 1490.0 nM 5.83 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 1 IC50 = 3614.0 nM 5.44 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 1 IC50 = 3614.0 nM 5.44 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -

Data from ChEMBL 36 via Core Engine