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Compound Detail

CHEMBL4633593

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CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O

Basic Information

ChEMBL ID CHEMBL4633593
Phase Preclinical
Structure Type MOL
InChI Key TYUDOPVEMCACJG-LBBUGJAGSA-N
2
Targets
19
Activities
2
Assay Types
2
PK Parameters
15
Publications
0
Known Names

Molecular Properties

967.1
MW (Da)
-2.87
ALogP
12
HBA
18
HBD
443.9
PSA (Ų)
0.02
QED
3
Ro5 Violations
30
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C44H70N16O9
MW 967.15
Aromatic Rings 2
Heavy Atoms 69
NP-Likeness 0.11

Activity Summary

EC50 12 meas. best 6.98
Ki 7 meas. best 8.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neuropeptide Y receptor type 4
CHEMBL4877
Ki 8.47 8.462 3.4 5
Neuropeptide Y receptor type 4
CHEMBL4877
EC50 6.98 6.84 104.7 12
P2Y purinoceptor 1
CHEMBL4315
Ki 5.93 5.93 1174.9 2

Pharmacokinetic Data

Parameter Value Units Species
T1/2 2.0 hr Homo sapiens
T1/2 1.4 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neuropeptide Y receptor type 4 Ki = 3.4 nM 8.47 Displacement of [3H]UR-KK200 from human Y4 receptor expressed in CHO-Gqi5-mtAQE ... 37440703
Neuropeptide Y receptor type 4 Ki = 3.4 nM 8.47 Displacement of [3H]UR-KK200 from human Y4 receptor expressed in CHO cells co-ex... 32614182
Neuropeptide Y receptor type 4 Ki = 3.388 nM 8.47 Displacement of [3H]UR-KK200 from human neuropeptide Y Y4 receptor expressed in ... 34748345
Neuropeptide Y receptor type 4 Ki = 3.388 nM 8.47 Displacement of [3H]UR-KK200 from human Y4 receptor expressed in CHO-Gqi5-mtAQE ... 37440703
Neuropeptide Y receptor type 4 Ki = 3.715 nM 8.43 Displacement of [3H]UR-KK200 from human Y4 receptor expressed in CHO cells co-ex... 32614182
Neuropeptide Y receptor type 4 EC50 = 104.71 nM 6.98 Agonist potency at human Y4 receptor expressed in HEK293T-NlucN-mGSi/Y4R-NlucC c... 37440703
Neuropeptide Y receptor type 4 EC50 = 110.0 nM 6.96 Agonist potency at human Y4 receptor expressed in HEK293T-NlucN-mGSi/Y4R-NlucC c... 37440703
Neuropeptide Y receptor type 4 EC50 = 112.2 nM 6.95 Agonist activity at human Y4R expressed in HEK293T cells co-expressing ARRB2 ass... 32614182
Neuropeptide Y receptor type 4 EC50 = 112.2 nM 6.95 Agonist activity at human neuropeptide Y Y4 receptor expressed in HEK293T-ARRB2 ... 34748345
Neuropeptide Y receptor type 4 EC50 = 120.0 nM 6.92 Agonist activity at human Y4R expressed in HEK293T cells co-expressing ARRB2 ass... 32614182
Neuropeptide Y receptor type 4 EC50 = 162.18 nM 6.79 Agonist activity at human Y4R expressed in HEK293T cells co-expressing ARRB1 ass... 32614182
Neuropeptide Y receptor type 4 EC50 = 162.18 nM 6.79 Agonist activity at human neuropeptide Y Y4 receptor expressed in HEK293T-ARRB1 ... 34748345
Neuropeptide Y receptor type 4 EC50 = 170.0 nM 6.77 Agonist activity at human Y4R expressed in HEK293T cells co-expressing ARRB1 ass... 32614182
Neuropeptide Y receptor type 4 EC50 = 170.0 nM 6.77 Agonist activity at human neuropeptide Y Y4 receptor expressed in HEK293T-ARRB1 ... 34748345
Neuropeptide Y receptor type 4 EC50 = 181.97 nM 6.74 Agonist activity at human Y4 receptor expressed in CHO cells co-expressing Gqi5-... 32614182
Neuropeptide Y receptor type 4 EC50 = 181.97 nM 6.74 Agonist activity at human neuropeptide Y Y4 receptor expressed in CHO-mtAEQ cell... 34748345
Neuropeptide Y receptor type 4 EC50 = 190.0 nM 6.72 Agonist activity at human Y4 receptor expressed in CHO cells co-expressing Gqi5-... 32614182
P2Y purinoceptor 1 Ki = 1174.9 nM 5.93 Displacement of [3H]UR-MK299 from human Y1 receptor expressed in human SK-N-MC c... 37440703
P2Y purinoceptor 1 Ki = 1180.0 nM 5.93 Displacement of [3H]UR-MK299 from human Y1 receptor expressed in human SK-N-MC c... 37440703

Literature References

PubMed DOI Target Context # Activities
34748345 10.1021/acs.jmedchem.1c01574 Neuropeptide Y receptor type 4 9
32614182 10.1021/acs.jmedchem.0c00426 Neuropeptide Y receptor type 4 8
37440703 10.1021/acs.jmedchem.3c00363 Neuropeptide Y receptor type 4 5
32614182 10.1021/acs.jmedchem.0c00426 Unchecked 3
34748345 10.1021/acs.jmedchem.1c01574 Unchecked 3
37440703 10.1021/acs.jmedchem.3c00363 ADMET 3
32614182 10.1021/acs.jmedchem.0c00426 Neuropeptide Y receptor type 1 2
32614182 10.1021/acs.jmedchem.0c00426 Neuropeptide Y receptor type 2 2
32614182 10.1021/acs.jmedchem.0c00426 Neuropeptide Y receptor type 5 2
34748345 10.1021/acs.jmedchem.1c01574 Neuropeptide Y receptor type 1 2
34748345 10.1021/acs.jmedchem.1c01574 Neuropeptide Y receptor type 2 2
34748345 10.1021/acs.jmedchem.1c01574 Neuropeptide Y receptor type 5 2
37440703 10.1021/acs.jmedchem.3c00363 P2Y purinoceptor 1 2
37440703 10.1021/acs.jmedchem.3c00363 Neuropeptide Y receptor type 2 2
37440703 10.1021/acs.jmedchem.3c00363 Neuropeptide Y receptor type 5 2

Data from ChEMBL 36 via Core Engine