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Compound Detail

CHEMBL213207

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c1cnc2[nH]cc(-c3ccnc(NCC4CCCCC4)n3)c2c1

Basic Information

ChEMBL ID CHEMBL213207
Phase Preclinical
Structure Type MOL
InChI Key KEBXAEFZLCNLJJ-UHFFFAOYSA-N
12
Targets
12
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

307.4
MW (Da)
4.01
ALogP
4
HBA
2
HBD
66.5
PSA (Ų)
0.76
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H21N5
MW 307.40
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness -0.97

Activity Summary

Ki 9 meas. best 8.4
IC50 3 meas. best 6.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 2
CHEMBL301
Ki 8.4 8.4 4.0 1
Rho-associated protein kinase 2
CHEMBL2973
Ki 8.2 8.2 6.3 1
Cell division cycle 7-related protein kinase
CHEMBL5443
Ki 8.1 8.1 7.9 1
Homeodomain-interacting protein kinase 2
CHEMBL4576
Ki 7.8 7.8 15.8 1
Mitogen-activated protein kinase kinase kinase kinase 4
CHEMBL6166
Ki 7.7 7.7 19.9 1
MAP kinase-interacting serine/threonine-protein kinase 2
CHEMBL4204
Ki 7.1 7.1 79.4 1
Glycogen synthase kinase-3 beta
CHEMBL262
Ki 6.9 6.9 125.9 1
Cyclin-dependent kinase 1/cyclin B
CHEMBL2094127
IC50 6.82 6.82 151.0 1
cAMP-dependent protein kinase catalytic subunit alpha
CHEMBL4101
Ki 6.7 6.7 199.5 1
Interleukin-1 receptor-associated kinase 4
CHEMBL3778
Ki 6.5 6.5 316.2 1
HeLa
CHEMBL399
IC50 6.43 6.43 368.0 1
Proto-oncogene tyrosine-protein kinase receptor Ret
CHEMBL2041
IC50 4.0 4.0 100000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 2 Ki = 3.981 nM 8.4 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Rho-associated protein kinase 2 Ki = 6.31 nM 8.2 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Cell division cycle 7-related protein kinase Ki = 7.943 nM 8.1 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Homeodomain-interacting protein kinase 2 Ki = 15.85 nM 7.8 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Mitogen-activated protein kinase kinase kinase kinase 4 Ki = 19.95 nM 7.7 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
MAP kinase-interacting serine/threonine-protein kinase 2 Ki = 79.43 nM 7.1 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Glycogen synthase kinase-3 beta Ki = 125.89 nM 6.9 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Cyclin-dependent kinase 1/cyclin B IC50 = 151.0 nM 6.82 Inhibition of CDK1/cyclinB by Flashplate assay 16870444
cAMP-dependent protein kinase catalytic subunit alpha Ki = 199.53 nM 6.7 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Interleukin-1 receptor-associated kinase 4 Ki = 316.23 nM 6.5 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
HeLa IC50 = 368.0 nM 6.43 Antiproliferative activity against human HeLa cell line assessed as incorporatio... 16870444
Proto-oncogene tyrosine-protein kinase receptor Ret IC50 = 100000.0 nM 4.0 Inhibition of RET kinase 21724393

Literature References

PubMed DOI Target Context # Activities
16870444 10.1016/j.bmcl.2006.06.073 Cyclin-dependent kinase 1/cyclin B 1
16870444 10.1016/j.bmcl.2006.06.073 HeLa 1
21724393 10.1016/j.bmcl.2011.06.003 Proto-oncogene tyrosine-protein kinase receptor Ret 1

Data from ChEMBL 36 via Core Engine