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Compound Detail

CHEMBL6014795

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Cc1nc2c(F)cc(-c3nc(Nc4ccc5c(n4)CCN(C(=O)C4CCCN4)C5)ncc3F)cc2n1C1CC1

Basic Information

ChEMBL ID CHEMBL6014795
Phase Preclinical
Structure Type MOL
InChI Key QXBRBWDRQIISAT-UHFFFAOYSA-N
6
Targets
16
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

530.6
MW (Da)
4.19
ALogP
8
HBA
2
HBD
100.9
PSA (Ų)
0.40
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H28F2N8O
MW 530.58
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -1.22

Activity Summary

IC50 16 meas. best 8.87

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 4
CHEMBL331
IC50 8.87 8.85 1.4 3
Cyclin-dependent kinase 6
CHEMBL2508
IC50 8.43 8.3567 3.8 3
Cyclin-dependent kinase 9
CHEMBL3116
IC50 7.58 7.2267 26.6 3
Cyclin-dependent kinase 2
CHEMBL301
IC50 6.67 6.67 212.0 1
Cyclin-dependent kinase 1
CHEMBL308
IC50 6.63 6.5033 232.0 3
Cyclin-dependent kinase 7
CHEMBL3055
IC50 6.25 6.0633 556.0 3

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 4 IC50 = 1.35 nM 8.87 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 4 IC50 = 1.35 nM 8.87 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 4 IC50 = 1.53 nM 8.81 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 6 IC50 = 3.75 nM 8.43 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 6 IC50 = 3.75 nM 8.43 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 6 IC50 = 6.24 nM 8.21 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 9 IC50 = 26.6 nM 7.58 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 9 IC50 = 89.0 nM 7.05 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 9 IC50 = 89.0 nM 7.05 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 2 IC50 = 212.0 nM 6.67 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 1 IC50 = 232.0 nM 6.63 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 1 IC50 = 360.0 nM 6.44 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 1 IC50 = 360.0 nM 6.44 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 7 IC50 = 556.0 nM 6.25 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 7 IC50 = 1076.0 nM 5.97 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 7 IC50 = 1076.0 nM 5.97 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -

Data from ChEMBL 36 via Core Engine