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Compound Detail

CHEMBL3559801

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CC(C)(C)c1ccc(OC2CCCCC2O)cc1

Basic Information

ChEMBL ID CHEMBL3559801
Phase Preclinical
Structure Type MOL
InChI Key FTIXUILRMBSXNS-UHFFFAOYSA-N
4
Targets
20
Activities
2
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

248.4
MW (Da)
3.67
ALogP
2
HBA
1
HBD
29.5
PSA (Ų)
0.87
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C16H24O2
MW 248.37
Aromatic Rings 1
Heavy Atoms 18
NP-Likeness 0.34

Activity Summary

EC50 17 meas. best 10.52
Ki 3 meas. best 10.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neuropeptide Y receptor type 4
CHEMBL4877
EC50 10.52 7.8986 0.0 14
Neuropeptide Y receptor type 1
CHEMBL4777
EC50 10.4 10.4 0.0 1
Neuropeptide Y receptor type 2
CHEMBL4018
EC50 10.2 10.2 0.1 1
Neuropeptide Y receptor type 4
CHEMBL4877
Ki 10.2 8.8667 0.1 3
Neuropeptide Y receptor type 5
CHEMBL4561
EC50 8.5 8.5 3.2 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neuropeptide Y receptor type 4 EC50 = 0.03 nM 10.52 Positive allosteric modulation of human NY4 receptor expressed in African green ... 28795803
Neuropeptide Y receptor type 4 EC50 = 0.03981 nM 10.4 Positive allosteric modulation of human NY4 receptor expressed in African green ... 28795803
Neuropeptide Y receptor type 1 EC50 = 0.03981 nM 10.4 Positive allosteric modulation of human C-terminal eYFP-fused human NY1 receptor... 28795803
Neuropeptide Y receptor type 2 EC50 = 0.0631 nM 10.2 Positive allosteric modulation of human C-terminal eYFP-fused human NY2 receptor... 28795803
Neuropeptide Y receptor type 4 Ki = 0.0631 nM 10.2 Effect on pancreatic polypeptide-mediated displacement of 125I-pancreatic polype... 28795803
Neuropeptide Y receptor type 4 EC50 = 0.3981 nM 9.4 Positive allosteric modulation of human NY4 receptor expressed in African green ... 28795803
Neuropeptide Y receptor type 4 EC50 = 0.4 nM 9.4 Positive allosteric modulation of human NY4 receptor expressed in African green ... 28795803
Neuropeptide Y receptor type 4 EC50 = 0.5012 nM 9.3 Positive allosteric modulation of human NY4 receptor expressed in African green ... 28795803
Neuropeptide Y receptor type 4 EC50 = 0.5 nM 9.3 Positive allosteric modulation of human NY4 receptor expressed in African green ... 28795803
Neuropeptide Y receptor type 5 EC50 = 3.162 nM 8.5 Positive allosteric modulation of human C-terminal eYFP-fused human NY5 receptor... 28795803
Neuropeptide Y receptor type 4 EC50 = 3.981 nM 8.4 Positive allosteric modulation of human C-terminal eYFP-tagged NY4 receptor expr... 28795803
Neuropeptide Y receptor type 4 EC50 = 4.5 nM 8.35 Positive allosteric modulation of human C-terminal eYFP-tagged NY4 receptor expr... 28795803
Neuropeptide Y receptor type 4 Ki = 6.31 nM 8.2 Effect on neuropeptide Y-mediated displacement of 125I-pancreatic polypeptide fr... 28795803
Neuropeptide Y receptor type 4 Ki = 6.31 nM 8.2 Effect on peptide YY-mediated displacement of 125I-pancreatic polypeptide from h... 28795803
Neuropeptide Y receptor type 4 EC50 = 398.11 nM 6.4 Positive allosteric modulation of human C-terminal eYFP-tagged NY4 receptor expr... 28795803
Neuropeptide Y receptor type 4 EC50 = 443.0 nM 6.35 Positive allosteric modulation of human C-terminal eYFP-tagged NY4 receptor expr... 28795803
Neuropeptide Y receptor type 4 EC50 = 794.33 nM 6.1 Positive allosteric modulation of human C-terminal eYFP-tagged NY4 receptor expr... 28795803
Neuropeptide Y receptor type 4 EC50 = 845.0 nM 6.07 Positive allosteric modulation of human C-terminal eYFP-tagged NY4 receptor expr... 28795803
Neuropeptide Y receptor type 4 EC50 = 5011.87 nM 5.3 Positive allosteric modulation of human C-terminal eYFP-fused human NY4 receptor... 28795803
Neuropeptide Y receptor type 4 EC50 = 5100.0 nM 5.29 Positive allosteric modulation of human C-terminal eYFP-fused human NY4 receptor... 28795803

Literature References

PubMed DOI Target Context # Activities
28795803 10.1021/acs.jmedchem.7b00976 Neuropeptide Y receptor type 4 46
28795803 10.1021/acs.jmedchem.7b00976 Neuropeptide Y receptor type 1/2 2
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
28795803 10.1021/acs.jmedchem.7b00976 Neuropeptide Y receptor type 1 1
28795803 10.1021/acs.jmedchem.7b00976 Neuropeptide Y receptor type 2 1
28795803 10.1021/acs.jmedchem.7b00976 Neuropeptide Y receptor type 5 1
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 1

Data from ChEMBL 36 via Core Engine