Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL438945

HUMAN NEUROPEPTIDE Y
Phase I
Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
Phase I
CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)[C@@H](C)CC

Basic Information

ChEMBL ID CHEMBL438945
Name HUMAN NEUROPEPTIDE Y
Phase Phase I
Structure Type BOTH
InChI Key XKWCTHKJQNUFOQ-HRPSIEBRSA-N

Known Names

Human neuropeptide y
5
Targets
21
Activities
3
Assay Types
3
PK Parameters
20
Publications
1
Known Names
1
Indications

Molecular Properties

4271.8
MW (Da)

Drug Information

Molecule Type Protein
Chirality Single Enantiomer
USAN Stem -tide

Extended Properties

Molecular Formula C189H285N55O57S
MW 4271.75

Indications

Stress Disorders, Post-Traumatic

Activity Summary

IC50 13 meas. best 10.55
Ki 7 meas. best 10.12
EC50 1 meas. best 6.38

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neuropeptide Y receptor type 2
CHEMBL4018
IC50 10.55 9.905 0.0 4
Neuropeptide Y receptor type 1
CHEMBL4777
IC50 10.15 9.475 0.1 6
Neuropeptide Y receptor type 2
CHEMBL4018
Ki 10.12 9.61 0.1 2
Neuropeptide Y receptor type 1
CHEMBL4777
Ki 10.02 9.6667 0.1 3
Neuropeptide Y receptor type 5
CHEMBL4561
Ki 8.66 8.66 2.2 1
Neuropeptide Y receptor type 5
CHEMBL4561
IC50 8.52 8.52 3.0 1
Rattus norvegicus
CHEMBL376
IC50 8.39 7.875 4.1 2
Neuropeptide Y receptor type 4
CHEMBL4877
Ki 6.55 6.55 282.0 1
Neuropeptide Y receptor type 4
CHEMBL4877
EC50 6.38 6.38 417.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.3 hr Homo sapiens
T1/2 4.8 hr Homo sapiens
T1/2 0.2 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neuropeptide Y receptor type 2 IC50 = 0.028 nM 10.55 Displacement of [125I]peptide YY from Y2 receptor in human KAN-TS cells measured... 27876250
Neuropeptide Y receptor type 1 IC50 = 0.07 nM 10.15 Binding affinity to human neuropeptide Y1 receptor by radioligand displacement a... 23582449
Neuropeptide Y receptor type 2 Ki = 0.076 nM 10.12 Binding affinity to human neuropeptide Y receptor type 2 by radioligand displace... 23466604
Neuropeptide Y receptor type 2 IC50 = 0.09 nM 10.05 Binding affinity to human neuropeptide Y2 receptor by radioligand displacement a... 23582449
Neuropeptide Y receptor type 1 Ki = 0.096 nM 10.02 Binding affinity to human neuropeptide Y receptor type 1 by radioligand displace... 23466604
Neuropeptide Y receptor type 1 IC50 = 0.14 nM 9.85 Binding affinity to human neuropeptide Y receptor type 1 by radioligand displace... 23466604
Neuropeptide Y receptor type 2 IC50 = 0.19 nM 9.72 Binding affinity to human neuropeptide Y receptor type 2 by radioligand displace... 23466604
Neuropeptide Y receptor type 1 IC50 = 0.21 nM 9.68 Displacement of [125I]peptide YY from Y1 receptor in human SK-N-MC cells measure... 27876250
Neuropeptide Y receptor type 1 Ki = 0.21 nM 9.68 Displacement of [125I]Peptide YY from neuropeptide Y receptor type 1 in human SK... 23403082
Neuropeptide Y receptor type 1 IC50 = 0.22 nM 9.66 Displacement of [125I]Peptide YY from neuropeptide Y receptor type 1 in human SK... 23403082
Neuropeptide Y receptor type 2 IC50 = 0.5 nM 9.3 Compound was evaluated for its inhibitory activity against Y2 receptor of rabbit... -
Neuropeptide Y receptor type 1 Ki = 0.5 nM 9.3 Displacement of Cy5-pNPY from human Y1 receptor expressed in HEL cells after 90 ... 24090364
Neuropeptide Y receptor type 2 Ki = 0.8 nM 9.1 Displacement of Cy5-pNPY from human Y2 receptor expressed in CHO cells after 90 ... 24090364
Neuropeptide Y receptor type 1 IC50 = 1.2 nM 8.92 Inhibition of neuropeptide Y1 receptor in human SK-N-MC cells after 60 mins by s... 19916528
Neuropeptide Y receptor type 5 Ki = 2.2 nM 8.66 Displacement of Cy5-pNPY from human Y5 receptor expressed in human HEC-1B cells ... 24090364
Neuropeptide Y receptor type 1 IC50 = 2.6 nM 8.59 Displacement of [125I]-NPY from Y1 receptor in human MCF7 cells in presence of 1... 23265893
Neuropeptide Y receptor type 5 IC50 = 3.0 nM 8.52 Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell m... 10669561
Rattus norvegicus IC50 = 4.1 nM 8.39 The concentration of peptide producing a 50% inhibition of the maximum binding i... 2342055
Rattus norvegicus IC50 = 44.0 nM 7.36 The concentration of peptide producing a 50% inhibition of the maximum effect in... 2342055
Neuropeptide Y receptor type 4 Ki = 282.0 nM 6.55 Displacement of Cy5-[K4]hPP from human Y4 receptor expressed in CHO cells after ... 24090364

Literature References

PubMed DOI Target Context # Activities
2342055 10.1021/jm00168a014 Rattus norvegicus 4
23403082 10.1016/j.bmcl.2013.01.025 Neuropeptide Y receptor type 1 3
24090364 10.1021/jm4008505 Neuropeptide Y receptor type 4 3
24044354 10.1021/jm400423p Xaa-Pro aminopeptidase 2 2
23466604 10.1016/j.ejmech.2013.01.044 Neuropeptide Y receptor type 2 2
23466604 10.1016/j.ejmech.2013.01.044 Neuropeptide Y receptor type 1 2
27876250 10.1016/j.bmc.2016.11.014 Neuropeptide Y receptor type 2 1
24044354 10.1021/jm400423p Neuropeptide Y receptor type 1 1
24044354 10.1021/jm400423p Prolyl endopeptidase FAP 1
24044354 10.1021/jm400423p Dipeptidyl peptidase 8 1
24044354 10.1021/jm400423p Neuropeptide Y receptor type 2 1
24090364 10.1021/jm4008505 Neuropeptide Y receptor type 1 1
24090364 10.1021/jm4008505 Neuropeptide Y receptor type 2 1
24090364 10.1021/jm4008505 Neuropeptide Y receptor type 5 1
23582449 10.1016/j.bmc.2013.03.016 Neuropeptide Y receptor type 1 1
23582449 10.1016/j.bmc.2013.03.016 Neuropeptide Y receptor type 2 1
23265893 10.1016/j.bmcl.2012.11.110 Neuropeptide Y receptor type 1 1
19916528 10.1021/np900287e Neuropeptide Y receptor type 1 1
- 10.1016/S0960-894X(00)80696-4 Rattus norvegicus 1
- 10.1016/S0960-894X(00)80696-4 Neuropeptide Y receptor type 2 1

Data from ChEMBL 36 via Core Engine