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Compound Detail

CHEMBL439904

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CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)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(C)C

Basic Information

ChEMBL ID CHEMBL439904
Phase Preclinical
Structure Type BOTH
InChI Key AUHJXHCVECGTKR-DQNUUZSMSA-N
4
Targets
23
Activities
3
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

4049.5
MW (Da)

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C180H279N53O54
MW 4049.53

Activity Summary

EC50 17 meas. best 9.7
IC50 3 meas. best 9.24
Ki 3 meas. best 9.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neuropeptide Y receptor type 2
CHEMBL4018
EC50 9.7 9.255 0.2 8
Neuropeptide Y receptor type 2
CHEMBL4018
Ki 9.4 9.4 0.4 1
Neuropeptide Y receptor type 2
CHEMBL4018
IC50 9.24 8.76 0.6 3
Neuropeptide Y receptor type 1
CHEMBL4777
EC50 8.25 7.0867 5.6 3
Neuropeptide Y receptor type 5
CHEMBL4561
EC50 8.09 7.3367 8.2 3
Neuropeptide Y receptor type 5
CHEMBL4561
Ki 7.7 7.7 20.0 1
Neuropeptide Y receptor type 1
CHEMBL4777
Ki 7.68 7.68 21.0 1
Neuropeptide Y receptor type 4
CHEMBL4877
EC50 6.85 6.1 141.0 3

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neuropeptide Y receptor type 2 EC50 = 0.2 nM 9.7 Agonist activity at human NPY2R expressed in HEK293 cells co-transfected with CR... 32844654
Neuropeptide Y receptor type 2 EC50 = 0.28 nM 9.55 Agonist activity at human Y2 receptor expressed in CHO cell membranes after 120 ... 28684122
Neuropeptide Y receptor type 2 EC50 = 0.28 nM 9.55 Agonist activity at human neuropeptide Y2 receptor expressed in CHO cell membran... 28917449
Neuropeptide Y receptor type 2 EC50 = 0.3 nM 9.52 Agonist activity at human NPY2 receptor expressed in human KAN-TS cells by [35S]... 17055726
Neuropeptide Y receptor type 2 Ki = 0.4 nM 9.4 Displacement of human [125I]PYY from NPY2 receptor expressed in human KAN-TS cel... 17055726
Neuropeptide Y receptor type 2 IC50 = 0.57 nM 9.24 Displacement of [125I]-PYY from human neuropeptide Y2 receptor expressed in CHO ... 28917449
Neuropeptide Y receptor type 2 IC50 = 0.57 nM 9.24 Displacement of [125I]peptide YY from human Y2 receptor expressed in CHO cell me... 28684122
Neuropeptide Y receptor type 2 EC50 = 1.0 nM 9.0 Agonist activity at human NPYY2 receptor expressed in HEK293 cells assessed as d... 24900634
Neuropeptide Y receptor type 2 EC50 = 1.0 nM 9.0 Agonist activity at human NPY2R expressed in CHO cells assessed as inhibition of... 32844654
Neuropeptide Y receptor type 2 EC50 = 1.2 nM 8.92 Agonist activity at human NPY2R expressed in CHO cells assessed as inhibition of... 32844654
Neuropeptide Y receptor type 2 EC50 = 1.6 nM 8.8 Agonist activity at human Y2R expressed in HEK293 cells by FLIPR assay 36571995
Neuropeptide Y receptor type 1 EC50 = 5.6 nM 8.25 Agonist activity at human NPYY1 receptor expressed in HEK293 cells assessed as d... 24900634
Neuropeptide Y receptor type 5 EC50 = 8.2 nM 8.09 Agonist activity at human NPYY5 receptor expressed in HEK293 cells assessed as d... 24900634
Neuropeptide Y receptor type 2 IC50 = 16.0 nM 7.8 Agonist activity at human NPY2R expressed in HEK293 cells assessed as inhibition... 33449689
Neuropeptide Y receptor type 5 Ki = 20.0 nM 7.7 Displacement of [125I]PYY from NPY5 receptor expressed in human HEK293 cells 17055726
Neuropeptide Y receptor type 1 Ki = 21.0 nM 7.68 Displacement of [125I]PYY from NPY1 receptor expressed in human SK-N-MC cells 17055726
Neuropeptide Y receptor type 5 EC50 = 29.7 nM 7.53 Agonist activity at human Y5R expressed in HEK293 cells by FLIPR assay 36571995
Neuropeptide Y receptor type 1 EC50 = 48.9 nM 7.31 Agonist activity at human Y1R expressed in HEK293 cells by FLIPR assay 36571995
Neuropeptide Y receptor type 4 EC50 = 141.0 nM 6.85 Agonist activity at human NPYY4 receptor expressed in HEK293 cells assessed as d... 24900634
Neuropeptide Y receptor type 5 EC50 = 410.0 nM 6.39 Agonist activity at NPY5R (unknown origin) by CRE-luciferase reporter gene assay 32844654

Literature References

PubMed DOI Target Context # Activities
28917449 10.1016/j.bmc.2017.08.044 Mus musculus 10
28684122 10.1016/j.bmcl.2017.06.055 Mus musculus 9
32844654 10.1021/acs.jmedchem.0c00740 Neuropeptide Y receptor type 2 4
33449689 10.1021/acs.jmedchem.0c01783 Unchecked 2
28684122 10.1016/j.bmcl.2017.06.055 Neuropeptide Y receptor type 2 2
28917449 10.1016/j.bmc.2017.08.044 Neuropeptide Y receptor type 2 2
17055726 10.1016/j.bmcl.2006.10.007 Neuropeptide Y receptor type 2 2
28917449 10.1016/j.bmc.2017.08.044 Homo sapiens 1
36571995 10.1016/j.ejmech.2022.115036 Neuropeptide Y receptor type 5 1
33449689 10.1021/acs.jmedchem.0c01783 Neuropeptide Y receptor type 1 1
33449689 10.1021/acs.jmedchem.0c01783 Neuropeptide Y receptor type 2 1
33449689 10.1021/acs.jmedchem.0c01783 Glucagon-like peptide 1 receptor 1
32844654 10.1021/acs.jmedchem.0c00740 Neuropeptide Y receptor type 1 1
32844654 10.1021/acs.jmedchem.0c00740 Neuropeptide Y receptor type 4 1
32844654 10.1021/acs.jmedchem.0c00740 Neuropeptide Y receptor type 5 1
24900634 10.1021/ml400335g Neuropeptide Y receptor type 1 1
24900634 10.1021/ml400335g Neuropeptide Y receptor type 2 1
24900634 10.1021/ml400335g Neuropeptide Y receptor type 4 1
24900634 10.1021/ml400335g Neuropeptide Y receptor type 5 1
17055726 10.1016/j.bmcl.2006.10.007 Neuropeptide Y receptor type 5 1

Data from ChEMBL 36 via Core Engine