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Compound Detail

CHEMBL5994564

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Cc1nc2c(F)cc(-c3nc(Nc4ccc5c(n4)CCN(C[C@@H]4CCCN4C)C5)ncc3F)cc2n1C1CC1

Basic Information

ChEMBL ID CHEMBL5994564
Phase Preclinical
Structure Type MOL
InChI Key DSMBDRWDECFDNR-NRFANRHFSA-N
7
Targets
14
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

530.6
MW (Da)
5.01
ALogP
8
HBA
1
HBD
75.0
PSA (Ų)
0.38
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H32F2N8
MW 530.63
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -1.22

Activity Summary

IC50 14 meas. best 9.04

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 4
CHEMBL331
IC50 9.04 9.04 0.9 2
Cyclin-dependent kinase 6
CHEMBL2508
IC50 8.85 8.85 1.4 2
Cyclin-dependent kinase 2
CHEMBL301
IC50 7.54 7.54 28.5 2
Cyclin-dependent kinase 7
CHEMBL3055
IC50 6.91 6.91 124.0 2
Cyclin-dependent kinase 9
CHEMBL3116
IC50 6.79 6.79 164.0 2
Cyclin-dependent kinase 5
CHEMBL4036
IC50 6.62 6.62 239.0 2
Cyclin-dependent kinase 1
CHEMBL308
IC50 5.98 5.98 1054.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 4 IC50 = 0.91 nM 9.04 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 4 IC50 = 0.91 nM 9.04 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 6 IC50 = 1.41 nM 8.85 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 6 IC50 = 1.41 nM 8.85 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 2 IC50 = 28.5 nM 7.54 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 2 IC50 = 28.5 nM 7.54 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 7 IC50 = 124.0 nM 6.91 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 7 IC50 = 124.0 nM 6.91 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 9 IC50 = 164.0 nM 6.79 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 9 IC50 = 164.0 nM 6.79 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 5 IC50 = 239.0 nM 6.62 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 5 IC50 = 239.0 nM 6.62 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -
Cyclin-dependent kinase 1 IC50 = 1054.0 nM 5.98 LANCE Ultra ULight Assay: 1. Take 10 mM stock solution of the test compound, in ... -
Cyclin-dependent kinase 1 IC50 = 1054.0 nM 5.98 Inhibitory Activity Assay: 1. Take 10 mM stock solution of the test compound, in... -

Data from ChEMBL 36 via Core Engine