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Compound Detail

CHEMBL4084419

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CCNC(=O)c1cc2c(N3CCOC[C@@H]3C)ccnc2n1C

Basic Information

ChEMBL ID CHEMBL4084419
Phase Preclinical
Structure Type MOL
InChI Key SYYSMZCCSNLTHZ-NSHDSACASA-N
3
Targets
6
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

302.4
MW (Da)
1.55
ALogP
5
HBA
1
HBD
59.4
PSA (Ų)
0.93
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 C16H22N4O2
MW 302.38
Aromatic Rings 2
Heavy Atoms 22
NP-Likeness -1.30

Activity Summary

Ki 6 meas. best 6.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; anion channel
CHEMBL1907607
Ki 6.72 6.685 190.6 2
Gamma-aminobutyric acid receptor subunit alpha-1
CHEMBL1962
Ki 6.65 6.65 224.0 1
D(4) dopamine receptor
CHEMBL219
Ki 6.15 6.1367 708.0 3

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL5724558 Colon cancer organoid 12
- 10.6019/CHEMBL5674860 Colon cancer organoid 12
- 10.6019/CHEMBL4689842 HEK-293T 10
- 10.6019/CHEMBL4689842 Fibroblast 10
- 10.6019/CHEMBL4689842 U2OS 9
- 10.6019/CHEMBL4507271 Unchecked 8
- 10.6019/CHEMBL5608141 Colon cancer organoid 6
- 10.1158/2159-8290.CD-23-0050 Colon cancer organoid 5
- 10.6019/CHEMBL4507271 GABA-A receptor; anion channel 4
- 10.6019/CHEMBL4507271 Muscarinic acetylcholine receptor M5 3
- 10.6019/CHEMBL4507271 Sodium-dependent serotonin transporter 3
- 10.6019/CHEMBL4507271 Sigma non-opioid intracellular receptor 1 3
- 10.6019/CHEMBL4507271 D(4) dopamine receptor 3
- 10.6019/CHEMBL4507271 Alpha-2A adrenergic receptor 1
- 10.6019/CHEMBL4507271 Alpha-2B adrenergic receptor 1
- 10.6019/CHEMBL4507271 Alpha-1D adrenergic receptor 1
- 10.6019/CHEMBL4507271 Alpha-1B adrenergic receptor 1
- 10.6019/CHEMBL4507271 Sodium-dependent dopamine transporter 1
- 10.1021/acschembio.2c00877 Colon organoid 1
- 10.6019/CHEMBL4507271 Beta-3 adrenergic receptor 1

Data from ChEMBL 36 via Core Engine