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Compound Detail

CHEMBL1774204

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N=C(N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(CNC(N)=O)cc1

Basic Information

ChEMBL ID CHEMBL1774204
Phase Preclinical
Structure Type MOL
InChI Key TVMJSGGZULFVCZ-XMMPIXPASA-N
4
Targets
6
Activities
2
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

529.6
MW (Da)
2.05
ALogP
4
HBA
7
HBD
175.2
PSA (Ų)
0.10
QED
2
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug Chemical Probe

Extended Properties

Molecular Formula C29H35N7O3
MW 529.65
Aromatic Rings 3
Heavy Atoms 39
NP-Likeness -0.40

Activity Summary

IC50 5 meas. best 9.42
Ki 1 meas. best 9.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neuropeptide Y receptor type 1
CHEMBL4777
Ki 9.6 9.6 0.2 1
Neuropeptide Y receptor type 1
CHEMBL4777
IC50 9.42 9.29 0.4 2
Neuropeptide Y receptor type 1
CHEMBL2587
IC50 9.14 9.14 0.7 1
Neuropeptide Y receptor type 4
CHEMBL4877
IC50 4.91 4.91 12300.0 1
Neuropeptide Y receptor type 5
CHEMBL2548
IC50 4.68 4.68 21000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL5463723 Unchecked 10
- 10.6019/CHEMBL5463723 Neuropeptide Y receptor type 2 4
- 10.6019/CHEMBL5463723 D(2) dopamine receptor 3
- 10.6019/CHEMBL5463723 Gamma-aminobutyric acid receptor subunit alpha-1 3
- 10.6019/CHEMBL5463723 D(1A) dopamine receptor 3
- 10.6019/CHEMBL5463723 Neuropeptide Y receptor type 1 3
- 10.6019/CHEMBL5463723 5-hydroxytryptamine receptor 1A 2
- 10.6019/CHEMBL5463723 Beta-2 adrenergic receptor 2
- 10.6019/CHEMBL5463723 Beta-1 adrenergic receptor 2
- 10.6019/CHEMBL5463723 Androgen receptor 2
- 10.6019/CHEMBL5463723 Alpha-2A adrenergic receptor 2
- 10.6019/CHEMBL5463723 Neuropeptide Y receptor type 5 2
- 10.6019/CHEMBL5463723 Adenosine receptor A2a 2
- 10.6019/CHEMBL5463723 Voltage-dependent L-type calcium channel subunit alpha-1C 2
- 10.6019/CHEMBL5463723 Endothelin-1 receptor 2
- 10.6019/CHEMBL5463723 Muscarinic acetylcholine receptor M1 2
- 10.6019/CHEMBL5463723 Kappa-type opioid receptor 2
- 10.6019/CHEMBL5463723 Glucocorticoid receptor 2
- 10.6019/CHEMBL5463723 Tyrosine-protein kinase Lck 2
24074877 10.1016/j.bmc.2013.08.065 Neuropeptide Y receptor type 4 2

Data from ChEMBL 36 via Core Engine