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Compound Detail

CHEMBL86066

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CC(C)n1cnc2c(NCc3ccccc3)nc(NCCO)nc21

Basic Information

ChEMBL ID CHEMBL86066
Phase Preclinical
Structure Type MOL
InChI Key WHDJEAZLMYPLGL-UHFFFAOYSA-N
9
Targets
13
Activities
2
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

326.4
MW (Da)
2.42
ALogP
7
HBA
3
HBD
87.9
PSA (Ų)
0.62
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H22N6O
MW 326.40
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -0.97

Activity Summary

Ki 9 meas. best 5.9
IC50 4 meas. best 5.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 5
CHEMBL4036
Ki 5.9 5.9 1258.9 1
Cyclin-dependent kinase 2
CHEMBL301
Ki 5.8 5.8 1584.9 1
Dual specificity protein kinase CLK2
CHEMBL4225
Ki 5.8 5.8 1584.9 1
Homeodomain-interacting protein kinase 4
CHEMBL1075167
Ki 5.7 5.7 1995.3 1
Cyclin-dependent kinase 1
CHEMBL308
IC50 5.7 5.365 2000.0 2
Casein kinase I isoform delta
CHEMBL2828
Ki 5.6 5.6 2511.9 1
Dual specificity protein kinase CLK4
CHEMBL4203
Ki 5.6 5.6 2511.9 1
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
CHEMBL2292
Ki 5.5 5.5 3162.3 1
SRSF protein kinase 1
CHEMBL4375
Ki 5.2 5.2 6309.6 1
Cyclin-dependent kinase 2
CHEMBL301
IC50 5.1 5.1 8000.0 1
Cyclin-dependent kinase 1
CHEMBL308
Ki 5.1 5.1 7943.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 5 Ki = 1258.93 nM 5.9 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Dual specificity protein kinase CLK2 Ki = 1584.89 nM 5.8 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Cyclin-dependent kinase 2 Ki = 1584.89 nM 5.8 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Cyclin-dependent kinase 1 IC50 = 2000.0 nM 5.7 Inhibitory activity against purified cdc2 p34/Cyclin B obtained from M phase ooc... 9046330
Homeodomain-interacting protein kinase 4 Ki = 1995.26 nM 5.7 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Casein kinase I isoform delta Ki = 2511.89 nM 5.6 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Dual specificity protein kinase CLK4 Ki = 2511.89 nM 5.6 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Dual specificity tyrosine-phosphorylation-regulated kinase 1A Ki = 3162.28 nM 5.5 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
SRSF protein kinase 1 Ki = 6309.57 nM 5.2 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Cyclin-dependent kinase 2 IC50 = 8000.0 nM 5.1 Inhibition of Cyclin-dependent kinase 2 10891109
Cyclin-dependent kinase 1 Ki = 7943.28 nM 5.1 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Cyclin-dependent kinase 1 IC50 = 9400.0 nM 5.03 Inhibition of Cyclin-dependent kinase 1 10891109

Literature References

PubMed DOI Target Context # Activities
25937014 10.1016/j.bmcl.2015.04.030 Unchecked 2
10891109 10.1021/jm990506w Cyclin-dependent kinase 1 1
10891109 10.1021/jm990506w Cyclin-dependent kinase 2 1
9046330 10.1021/jm960666x Cyclin-dependent kinase 1 1
24936234 10.1021/ml3002083 Voltage-dependent N-type calcium channel subunit alpha-1B 1
25937014 10.1016/j.bmcl.2015.04.030 BJ 1
36166733 10.1021/acs.jmedchem.2c00996 Plasmodium falciparum 1

Data from ChEMBL 36 via Core Engine