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Compound Detail

CHEMBL5950426

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

Basic Information

ChEMBL ID CHEMBL5950426
Phase Preclinical
Structure Type MOL
InChI Key IVKYJVDFJKEXIH-UHFFFAOYSA-N
6
Targets
12
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

561.6
MW (Da)
4.52
ALogP
8
HBA
1
HBD
95.3
PSA (Ų)
0.35
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H33F2N9O
MW 561.64
Aromatic Rings 4
Heavy Atoms 41
NP-Likeness -1.42

Activity Summary

IC50 12 meas. best 8.95

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 4
CHEMBL331
IC50 8.95 8.95 1.1 2
Cyclin-dependent kinase 6
CHEMBL2508
IC50 8.59 8.59 2.5 2
Cyclin-dependent kinase 9
CHEMBL3116
IC50 7.21 7.21 61.5 2
Cyclin-dependent kinase 1
CHEMBL308
IC50 6.46 6.46 348.0 2
Cyclin-dependent kinase 2
CHEMBL301
IC50 6.44 6.44 364.0 2
Cyclin-dependent kinase 7
CHEMBL3055
IC50 6.15 6.15 710.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 4 IC50 = 1.12 nM 8.95 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 4 IC50 = 1.12 nM 8.95 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 6 IC50 = 2.55 nM 8.59 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 6 IC50 = 2.55 nM 8.59 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 9 IC50 = 61.5 nM 7.21 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 9 IC50 = 61.5 nM 7.21 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 1 IC50 = 348.0 nM 6.46 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 1 IC50 = 348.0 nM 6.46 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 2 IC50 = 364.0 nM 6.44 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 2 IC50 = 364.0 nM 6.44 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 7 IC50 = 710.0 nM 6.15 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 7 IC50 = 710.0 nM 6.15 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -

Data from ChEMBL 36 via Core Engine