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Compound Detail

CHEMBL5872006

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Cc1nc2c(F)cc(-c3nc(Nc4ccc5c(n4)CCN(C[C@H]4CCCN4C)C5)ncc3F)cc2n1C1CC1

Basic Information

ChEMBL ID CHEMBL5872006
Phase Preclinical
Structure Type MOL
InChI Key DSMBDRWDECFDNR-OAQYLSRUSA-N
7
Targets
14
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

530.6
MW (Da)
5.01
ALogP
8
HBA
1
HBD
75.0
PSA (Ų)
0.38
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H32F2N8
MW 530.63
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -1.22

Activity Summary

IC50 14 meas. best 8.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 4
CHEMBL331
IC50 8.68 8.68 2.1 2
Cyclin-dependent kinase 6
CHEMBL2508
IC50 8.5 8.5 3.1 2
Cyclin-dependent kinase 5
CHEMBL4036
IC50 7.43 7.43 37.0 2
Cyclin-dependent kinase 7
CHEMBL3055
IC50 6.98 6.98 104.0 2
Cyclin-dependent kinase 9
CHEMBL3116
IC50 6.67 6.67 212.0 2
Cyclin-dependent kinase 2
CHEMBL301
IC50 6.5 6.5 317.0 2
Cyclin-dependent kinase 1
CHEMBL308
IC50 6.04 6.04 912.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 4 IC50 = 2.08 nM 8.68 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 4 IC50 = 2.08 nM 8.68 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 6 IC50 = 3.15 nM 8.5 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 6 IC50 = 3.15 nM 8.5 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 5 IC50 = 37.0 nM 7.43 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 5 IC50 = 37.0 nM 7.43 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 7 IC50 = 104.0 nM 6.98 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 7 IC50 = 104.0 nM 6.98 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 9 IC50 = 212.0 nM 6.67 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 9 IC50 = 212.0 nM 6.67 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 2 IC50 = 317.0 nM 6.5 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 2 IC50 = 317.0 nM 6.5 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 1 IC50 = 912.0 nM 6.04 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 1 IC50 = 912.0 nM 6.04 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -

Data from ChEMBL 36 via Core Engine