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Compound Detail

CHEMBL6002674

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CNCCN1CCc2nc(Nc3ncc(F)c(-c4cc(F)c5nc(C)n(C(C)(C)C)c5c4)n3)ccc2C1

Basic Information

ChEMBL ID CHEMBL6002674
Phase Preclinical
Structure Type MOL
InChI Key NCAQSQYHTSCOCV-UHFFFAOYSA-N
7
Targets
14
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

506.6
MW (Da)
4.55
ALogP
8
HBA
2
HBD
83.8
PSA (Ų)
0.40
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H32F2N8
MW 506.61
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -1.20

Activity Summary

IC50 14 meas. best 8.83

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 4
CHEMBL331
IC50 8.83 8.83 1.5 2
Cyclin-dependent kinase 6
CHEMBL2508
IC50 8.82 8.82 1.5 2
Cyclin-dependent kinase 2
CHEMBL301
IC50 8.18 8.18 6.7 2
Cyclin-dependent kinase 5
CHEMBL4036
IC50 8.08 8.08 8.4 2
Cyclin-dependent kinase 9
CHEMBL3116
IC50 7.98 7.98 10.5 2
Cyclin-dependent kinase 1
CHEMBL308
IC50 6.87 6.87 135.0 2
Cyclin-dependent kinase 7
CHEMBL3055
IC50 6.83 6.83 149.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 4 IC50 = 1.49 nM 8.83 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 4 IC50 = 1.49 nM 8.83 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 6 IC50 = 1.51 nM 8.82 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 6 IC50 = 1.51 nM 8.82 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 2 IC50 = 6.68 nM 8.18 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 2 IC50 = 6.68 nM 8.18 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 5 IC50 = 8.37 nM 8.08 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 5 IC50 = 8.37 nM 8.08 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 9 IC50 = 10.5 nM 7.98 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 9 IC50 = 10.5 nM 7.98 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 1 IC50 = 135.0 nM 6.87 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 1 IC50 = 135.0 nM 6.87 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 7 IC50 = 149.0 nM 6.83 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 7 IC50 = 149.0 nM 6.83 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -

Data from ChEMBL 36 via Core Engine