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Compound Detail

CHEMBL1682360

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c1cc2[nH]ncc2cc1-c1cc(CN2CCCCC2)no1

Basic Information

ChEMBL ID CHEMBL1682360
Phase Preclinical
Structure Type MOL
InChI Key ZTUKHYNMEWPBNZ-UHFFFAOYSA-N
15
Targets
16
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

282.4
MW (Da)
3.20
ALogP
4
HBA
1
HBD
58.0
PSA (Ų)
0.80
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H18N4O
MW 282.35
Aromatic Rings 3
Heavy Atoms 21
NP-Likeness -2.17

Activity Summary

Ki 16 meas. best 6.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Rho-associated protein kinase 2
CHEMBL2973
Ki 6.7 6.6 199.5 2
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
CHEMBL2292
Ki 6.2 6.2 631.0 1
Rho-associated protein kinase 1
CHEMBL3231
Ki 6.2 6.2 631.0 1
Death-associated protein kinase 3
CHEMBL2468
Ki 6.1 6.1 794.3 1
LIM domain kinase 1
CHEMBL3836
Ki 6.1 6.1 794.3 1
Cyclin-dependent kinase 2
CHEMBL301
Ki 6.0 6.0 1000.0 1
Serine/threonine-protein kinase Chk2
CHEMBL2527
Ki 5.9 5.9 1258.9 1
Glycogen synthase kinase-3 alpha
CHEMBL2850
Ki 5.7 5.7 1995.3 1
cAMP-dependent protein kinase catalytic subunit alpha
CHEMBL4101
Ki 5.6 5.6 2511.9 1
Aurora kinase A
CHEMBL4722
Ki 5.6 5.6 2511.9 1
Cyclin-dependent kinase 5
CHEMBL4036
Ki 5.5 5.5 3162.3 1
Glycogen synthase kinase-3 beta
CHEMBL262
Ki 5.42 5.42 3810.0 1
Cyclin-dependent kinase 1
CHEMBL308
Ki 5.3 5.3 5011.9 1
MAP/microtubule affinity-regulating kinase 3
CHEMBL5600
Ki 5.3 5.3 5011.9 1
Ribosomal protein S6 kinase alpha-3
CHEMBL2345
Ki 5.2 5.2 6309.6 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Rho-associated protein kinase 2 Ki = 199.53 nM 6.7 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Rho-associated protein kinase 2 Ki = 315.0 nM 6.5 Inhibition of Rock2 after 1 hr using biotinylated longS peptide as substrate 21282054
Dual specificity tyrosine-phosphorylation-regulated kinase 1A Ki = 630.96 nM 6.2 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Rho-associated protein kinase 1 Ki = 630.96 nM 6.2 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
LIM domain kinase 1 Ki = 794.33 nM 6.1 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Death-associated protein kinase 3 Ki = 794.33 nM 6.1 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Cyclin-dependent kinase 2 Ki = 1000.0 nM 6.0 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Serine/threonine-protein kinase Chk2 Ki = 1258.93 nM 5.9 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Glycogen synthase kinase-3 alpha Ki = 1995.26 nM 5.7 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Aurora kinase A Ki = 2511.89 nM 5.6 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
cAMP-dependent protein kinase catalytic subunit alpha Ki = 2511.89 nM 5.6 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Cyclin-dependent kinase 5 Ki = 3162.28 nM 5.5 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Glycogen synthase kinase-3 beta Ki = 3810.0 nM 5.42 Inhibition of GSK3-beta after 1 hr 21282054
MAP/microtubule affinity-regulating kinase 3 Ki = 5011.87 nM 5.3 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Cyclin-dependent kinase 1 Ki = 5011.87 nM 5.3 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Ribosomal protein S6 kinase alpha-3 Ki = 6309.57 nM 5.2 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -

Literature References

PubMed DOI Target Context # Activities
21282054 10.1016/j.bmcl.2011.01.007 Aurora kinase B 1
21282054 10.1016/j.bmcl.2011.01.007 Epidermal growth factor receptor 1
21282054 10.1016/j.bmcl.2011.01.007 Glycogen synthase kinase-3 beta 1
21282054 10.1016/j.bmcl.2011.01.007 Tyrosine-protein kinase JAK2 1
21282054 10.1016/j.bmcl.2011.01.007 Vascular endothelial growth factor receptor 2 1
21282054 10.1016/j.bmcl.2011.01.007 Serine/threonine-protein kinase PAK 4 1
21282054 10.1016/j.bmcl.2011.01.007 Serine/threonine-protein kinase pim-1 1
21282054 10.1016/j.bmcl.2011.01.007 Rho-associated protein kinase 2 1

Data from ChEMBL 36 via Core Engine