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Compound Detail

CHEMBL196258

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CCCCCc1nc(N)c2nc(-n3nccn3)n(C)c2n1

Basic Information

ChEMBL ID CHEMBL196258
Phase Preclinical
Structure Type MOL
InChI Key PYUBHJHQYILWFE-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

286.3
MW (Da)
1.26
ALogP
8
HBA
1
HBD
100.3
PSA (Ų)
0.71
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C13H18N8
MW 286.34
Aromatic Rings 3
Heavy Atoms 21
NP-Likeness -1.08

Activity Summary

Ki 4 meas. best 8.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adenosine receptor A2a
CHEMBL251
Ki 8.48 8.48 3.3 1
Adenosine receptor A1
CHEMBL226
Ki 7.58 7.58 26.2 1
Adenosine receptor A2b
CHEMBL255
Ki 6.82 6.82 153.0 1
Adenosine receptor A3
CHEMBL256
Ki 6.12 6.12 760.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16250647 10.1021/jm058018d GABA-A receptor; anion channel 2
16250647 10.1021/jm058018d Unchecked 2
16250647 10.1021/jm058018d Glutamate [NMDA] receptor 2
16250647 10.1021/jm058018d Adenosine receptors; A2a & A2b 1
16250647 10.1021/jm058018d Beta-1 adrenergic receptor 1
16250647 10.1021/jm058018d Adenosine receptor A2b 1
16250647 10.1021/jm058018d Muscarinic acetylcholine receptor M3 1
16250647 10.1021/jm058018d Muscarinic acetylcholine receptor M2 1
16250647 10.1021/jm058018d Muscarinic acetylcholine receptor M1 1
16250647 10.1021/jm058018d Histamine H1 receptor 1
16250647 10.1021/jm058018d Glutamate receptor ionotropic kainate 1
16250647 10.1021/jm058018d Glutamate receptor ionotropic AMPA 1
16250647 10.1021/jm058018d Adenosine receptor A2a 1
16250647 10.1021/jm058018d Sodium- and chloride-dependent GABA transporter 1 1
16250647 10.1021/jm058018d GABA-B receptor 1
16250647 10.1021/jm058018d D(1B) dopamine receptor 1
16250647 10.1021/jm058018d D(4) dopamine receptor 1
16250647 10.1021/jm058018d D(3) dopamine receptor 1
16250647 10.1021/jm058018d D(2) dopamine receptor 1
16250647 10.1021/jm058018d D(1A) dopamine receptor 1

Data from ChEMBL 36 via Core Engine