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Compound Detail

CHEMBL5759958

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Cc1nc2c(F)cc(-c3nc(Nc4ccc5c(n4)CCN(C(=O)CN(C)C)C5)ncc3F)cc2n1C1CCCC1

Basic Information

ChEMBL ID CHEMBL5759958
Phase Preclinical
Structure Type MOL
InChI Key ZFXSUJXETQKSKI-UHFFFAOYSA-N
6
Targets
12
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

546.6
MW (Da)
4.78
ALogP
8
HBA
1
HBD
92.1
PSA (Ų)
0.37
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H32F2N8O
MW 546.63
Aromatic Rings 4
Heavy Atoms 40
NP-Likeness -1.50

Activity Summary

IC50 12 meas. best 8.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 4
CHEMBL331
IC50 8.46 8.46 3.5 2
Cyclin-dependent kinase 6
CHEMBL2508
IC50 7.97 7.97 10.6 2
Cyclin-dependent kinase 9
CHEMBL3116
IC50 7.44 7.44 36.1 2
Cyclin-dependent kinase 1
CHEMBL308
IC50 6.74 6.74 183.0 2
Cyclin-dependent kinase 2
CHEMBL301
IC50 6.71 6.71 193.0 2
Cyclin-dependent kinase 7
CHEMBL3055
IC50 5.98 5.98 1045.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 4 IC50 = 3.49 nM 8.46 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 4 IC50 = 3.49 nM 8.46 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 6 IC50 = 10.6 nM 7.97 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 6 IC50 = 10.6 nM 7.97 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 9 IC50 = 36.1 nM 7.44 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 9 IC50 = 36.1 nM 7.44 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 1 IC50 = 183.0 nM 6.74 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 1 IC50 = 183.0 nM 6.74 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 2 IC50 = 193.0 nM 6.71 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 2 IC50 = 193.0 nM 6.71 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 7 IC50 = 1045.0 nM 5.98 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 7 IC50 = 1045.0 nM 5.98 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -

Data from ChEMBL 36 via Core Engine