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Compound Detail

CHEMBL407391

DIMETHYLADENINE
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CN(C)c1ncnc2nc[nH]c12

Basic Information

ChEMBL ID CHEMBL407391
Name DIMETHYLADENINE
Phase Preclinical
Structure Type MOL
InChI Key BVIAOQMSVZHOJM-UHFFFAOYSA-N
12
Targets
16
Activities
2
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

163.2
MW (Da)
0.42
ALogP
4
HBA
1
HBD
57.7
PSA (Ų)
0.66
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C7H9N5
MW 163.18
Aromatic Rings 2
Heavy Atoms 12
NP-Likeness -1.05

Activity Summary

Ki 12 meas. best 5.96
IC50 4 meas. best 5.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 2/cyclin E1
CHEMBL1907605
Ki 5.96 5.96 1096.5 1
Leucine-rich repeat serine/threonine-protein kinase 2
CHEMBL1075104
Ki 5.85 5.85 1425.0 1
Leucine-rich repeat serine/threonine-protein kinase 2
CHEMBL1075104
IC50 5.47 5.47 3355.0 1
Serine/threonine-protein kinase Chk2
CHEMBL2527
Ki 5.4 5.4 3981.1 1
Aurora kinase A
CHEMBL4722
Ki 5.4 5.4 3981.1 1
Ribosomal protein S6 kinase alpha-3
CHEMBL2345
Ki 5.3 5.3 5011.9 1
MAP/microtubule affinity-regulating kinase 3
CHEMBL5600
Ki 5.3 5.3 5011.9 1
3-phosphoinositide-dependent protein kinase 1
CHEMBL2534
Ki 5.1 5.1 7943.3 1
Serine/threonine-protein kinase MARK2
CHEMBL3831
Ki 5.1 5.1 7943.3 1
Protein kinase C delta type
CHEMBL2996
Ki 4.9 4.9 12589.2 1
Serine/threonine-protein kinase Chk1
CHEMBL4630
Ki 4.9 4.9 12589.2 1
cAMP-dependent protein kinase catalytic subunit alpha
CHEMBL4101
Ki 4.8 4.8 15848.9 1
Heat shock protein HSP90
CHEMBL2095165
IC50 2.82 2.82 1500000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 2/cyclin E1 Ki = 1096.48 nM 5.96 Inhibition of human recombinant CDK2/CycE using HHASPRK as substrate by ESI-MS a... 22289061
Leucine-rich repeat serine/threonine-protein kinase 2 Ki = 1425.0 nM 5.85 Binding affinity to human GST tagged truncated LRRK2 G2019S mutant incubated for... 34184879
Leucine-rich repeat serine/threonine-protein kinase 2 IC50 = 3355.0 nM 5.47 Inhibition of recombinant human GST tagged truncated LRRK2 G2019S mutant using f... 34184879
Aurora kinase A Ki = 3981.07 nM 5.4 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Serine/threonine-protein kinase Chk2 Ki = 3981.07 nM 5.4 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Ribosomal protein S6 kinase alpha-3 Ki = 5011.87 nM 5.3 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
MAP/microtubule affinity-regulating kinase 3 Ki = 5011.87 nM 5.3 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Serine/threonine-protein kinase MARK2 Ki = 7943.28 nM 5.1 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
3-phosphoinositide-dependent protein kinase 1 Ki = 7943.28 nM 5.1 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Protein kinase C delta type Ki = 12589.25 nM 4.9 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Serine/threonine-protein kinase Chk1 Ki = 12589.25 nM 4.9 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
cAMP-dependent protein kinase catalytic subunit alpha Ki = 15848.93 nM 4.8 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Heat shock protein HSP90 IC50 = 1500000.0 nM 2.82 Inhibition of HSP90 (unknown origin) by confocal fluorescence-based biochemical ... 32539387

Literature References

PubMed DOI Target Context # Activities
18077363 10.1073/pnas.0708800104 Serine/threonine-protein kinase 26 2
18077363 10.1073/pnas.0708800104 Ribosomal protein S6 kinase alpha-3 2
34184879 10.1021/acs.jmedchem.1c00720 Leucine-rich repeat serine/threonine-protein kinase 2 2
2165159 10.1021/jm00170a005 Phosphatidylinositol 4-kinase, PI4K 2
18077363 10.1073/pnas.0708800104 Calcium/calmodulin-dependent protein kinase type 1D 1
18077363 10.1073/pnas.0708800104 Cyclin-dependent kinase 2 1
18077363 10.1073/pnas.0708800104 Calcium/calmodulin-dependent protein kinase kinase 2 1
18077363 10.1073/pnas.0708800104 Calcium/calmodulin-dependent protein kinase type II subunit gamma 1
18077363 10.1073/pnas.0708800104 Calcium/calmodulin-dependent protein kinase type II subunit delta 1
18077363 10.1073/pnas.0708800104 Calcium/calmodulin-dependent protein kinase type II subunit beta 1
18077363 10.1073/pnas.0708800104 Calcium/calmodulin-dependent protein kinase type II subunit alpha 1
18077363 10.1073/pnas.0708800104 Calcium/calmodulin-dependent protein kinase type 1G 1
18077363 10.1073/pnas.0708800104 5'-AMP-activated protein kinase catalytic subunit alpha-2 1
- 10.6019/CHEMBL3301361 No relevant target 1
22289061 10.1021/jm200979x Protein-tyrosine kinase 2-beta 1
22289061 10.1021/jm200979x Tyrosine-protein kinase ZAP-70 1
22289061 10.1021/jm200979x Cyclin-dependent kinase 2/cyclin E1 1
21134755 10.1016/j.bmc.2010.11.004 Mitogen-activated protein kinase kinase kinase 5 1
18077363 10.1073/pnas.0708800104 HeLa 1
18077363 10.1073/pnas.0708800104 Unchecked 1

Data from ChEMBL 36 via Core Engine