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Compound Detail

CHEMBL5950534

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Cc1nc2c(F)cc(-c3nc(Nc4ccc5c(n4)C[C@@H](C)NC5)ncc3F)cc2n1C(C)(C)C

Basic Information

ChEMBL ID CHEMBL5950534
Phase Preclinical
Structure Type MOL
InChI Key JKKUZTDMJDZHEB-CYBMUJFWSA-N
7
Targets
28
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

463.5
MW (Da)
5.01
ALogP
7
HBA
2
HBD
80.5
PSA (Ų)
0.44
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H27F2N7
MW 463.54
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -0.70

Activity Summary

IC50 28 meas. best 8.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 4
CHEMBL331
IC50 8.96 8.88 1.1 4
Cyclin-dependent kinase 6
CHEMBL2508
IC50 8.53 8.47 3.0 4
Cyclin-dependent kinase 9
CHEMBL3116
IC50 8.26 8.205 5.4 4
Cyclin-dependent kinase 2
CHEMBL301
IC50 7.95 7.73 11.2 4
Cyclin-dependent kinase 5
CHEMBL4036
IC50 7.8 7.565 15.9 4
Cyclin-dependent kinase 1
CHEMBL308
IC50 7.26 7.02 55.1 4
Cyclin-dependent kinase 7
CHEMBL3055
IC50 7.0 6.99 99.4 4

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 4 IC50 = 1.09 nM 8.96 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 4 IC50 = 1.09 nM 8.96 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 4 IC50 = 1.59 nM 8.8 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 4 IC50 = 1.59 nM 8.8 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 6 IC50 = 2.98 nM 8.53 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 6 IC50 = 2.98 nM 8.53 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 6 IC50 = 3.86 nM 8.41 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 6 IC50 = 3.86 nM 8.41 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 9 IC50 = 5.44 nM 8.26 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 9 IC50 = 5.44 nM 8.26 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 9 IC50 = 7.03 nM 8.15 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 9 IC50 = 7.03 nM 8.15 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 2 IC50 = 11.2 nM 7.95 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 2 IC50 = 11.2 nM 7.95 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 5 IC50 = 15.9 nM 7.8 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 5 IC50 = 15.9 nM 7.8 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 2 IC50 = 30.7 nM 7.51 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 2 IC50 = 30.7 nM 7.51 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 5 IC50 = 47.2 nM 7.33 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 5 IC50 = 47.2 nM 7.33 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -

Data from ChEMBL 36 via Core Engine