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Compound Detail

CHEMBL5938059

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Cc1nc2c(F)cc(-c3nc(Nc4ccc5c(n4)CCN(CCN)C5)ncc3F)cc2n1C(C)(C)C

Basic Information

ChEMBL ID CHEMBL5938059
Phase Preclinical
Structure Type MOL
InChI Key IWSDTEGBQVXXON-UHFFFAOYSA-N
7
Targets
14
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

492.6
MW (Da)
4.29
ALogP
8
HBA
2
HBD
97.8
PSA (Ų)
0.43
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H30F2N8
MW 492.58
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -1.25

Activity Summary

IC50 14 meas. best 8.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 6
CHEMBL2508
IC50 8.96 8.96 1.1 2
Cyclin-dependent kinase 4
CHEMBL331
IC50 8.94 8.94 1.1 2
Cyclin-dependent kinase 5
CHEMBL4036
IC50 8.14 8.14 7.2 2
Cyclin-dependent kinase 9
CHEMBL3116
IC50 8.07 8.07 8.4 2
Cyclin-dependent kinase 2
CHEMBL301
IC50 7.68 7.68 20.8 2
Cyclin-dependent kinase 1
CHEMBL308
IC50 6.85 6.85 141.0 2
Cyclin-dependent kinase 7
CHEMBL3055
IC50 6.8 6.8 160.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 6 IC50 = 1.11 nM 8.96 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 6 IC50 = 1.11 nM 8.96 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 4 IC50 = 1.14 nM 8.94 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 4 IC50 = 1.14 nM 8.94 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 5 IC50 = 7.17 nM 8.14 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 5 IC50 = 7.17 nM 8.14 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 9 IC50 = 8.42 nM 8.07 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 9 IC50 = 8.42 nM 8.07 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 2 IC50 = 20.8 nM 7.68 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 2 IC50 = 20.8 nM 7.68 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 1 IC50 = 141.0 nM 6.85 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 1 IC50 = 141.0 nM 6.85 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 7 IC50 = 160.0 nM 6.8 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 7 IC50 = 160.0 nM 6.8 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -

Data from ChEMBL 36 via Core Engine