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Compound Detail

CHEMBL376756

KISSPEPTIN-10
🧪 Phase III
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🧪 Phase III
CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL376756
Name KISSPEPTIN-10
Phase Phase III
Structure Type BOTH
InChI Key RITKWYDZSSQNJI-INXYWQKQSA-N

Known Names

Human metastin 45-54 Kisspeptin-10 Kisspeptin-10 (human)
4
Targets
22
Activities
3
Assay Types
10
PK Parameters
20
Publications
3
Known Names
6
Indications

Molecular Properties

1302.5
MW (Da)

Drug Information

Molecule Type Protein
Chirality Single Enantiomer

Extended Properties

Molecular Formula C63H83N17O14
MW 1302.46

Indications

Infertility Hypogonadism Metabolic Diseases Paget Disease, Extramammary Polycystic Ovary Syndrome Pregnancy

Activity Summary

EC50 9 meas. best 10.31
IC50 7 meas. best 10.15
Ki 6 meas. best 10.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
KiSS-1 receptor
CHEMBL5413
 Ki 10.46 9.9925 0.0 4
KiSS-1 receptor
CHEMBL5413
 EC50 10.31 9.4257 0.0 7
KiSS-1 receptor
CHEMBL1169599
 Ki 10.24 10.15 0.1 2
KiSS-1 receptor
CHEMBL5413
 IC50 10.15 8.8075 0.1 4
KiSS-1 receptor
CHEMBL1169599
 IC50 9.96 9.96 0.1 1
KiSS-1 receptor
CHEMBL1169599
 EC50 8.38 8.38 4.2 2
Neuropeptide FF receptor 1
CHEMBL5951
 IC50 8.33 8.33 4.7 1
Neuropeptide FF receptor 2
CHEMBL5952
 IC50 7.12 7.12 76.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 1331.0 ng.hr.mL-1 Rattus norvegicus
AUC 1258.0 ng.hr.mL-1 Rattus norvegicus
CL 12.85 mL.min-1.kg-1 Rattus norvegicus
Cmax 539.75 nM Rattus norvegicus
F 94.5 % Rattus norvegicus
MRT 1.09 hr Rattus norvegicus
T1/2 0.009333 hr Mus musculus
T1/2 0.01667 hr Homo sapiens
T1/2 0.08333 hr Rattus norvegicus
Tmax 0.39 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
KiSS-1 receptor Ki = 0.035 nM 10.46 Displacement of radioligand from human KISS1R transfected in CHO cells 24918545
KiSS-1 receptor Ki = 0.039 nM 10.41 Binding affinity to human KISS1R expressed in CHO cell membranes 24047141
KiSS-1 receptor EC50 = 0.049 nM 10.31 Agonist activity at human KISS1R assessed as induction of intracellular calcium ... 22975302
KiSS-1 receptor Ki = 0.057 nM 10.24 Binding affinity to rat KISS1R 24047141
KiSS-1 receptor Ki = 0.062 nM 10.21 Displacement of [125I]-Kp-10 from human Kiss1 receptor by TopCount scintillation... 34008968
KiSS-1 receptor EC50 = 0.065 nM 10.19 Agonist activity at human OT7T175 assessed as increase in intracellular calcium ... 22995619
KiSS-1 receptor IC50 = 0.07 nM 10.15 Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membr... 19007202
KiSS-1 receptor IC50 = 0.082 nM 10.09 Binding affinity to human KISS1R 22975302
KiSS-1 receptor EC50 = 0.087 nM 10.06 Agonist activity at human KISS1R expressed in CHO cells assessed as increase in ... 30598349
KiSS-1 receptor Ki = 0.088 nM 10.06 Displacement of radioligand from rat KISS1R transfected in CHO cells 24918545
KiSS-1 receptor IC50 = 0.11 nM 9.96 Binding affinity to rat KISS1R 22975302
KiSS-1 receptor IC50 = 0.12 nM 9.92 Displacement of [125I]kisspeptin-15 from GPR54 24900254
KiSS-1 receptor EC50 = 0.24 nM 9.62 Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kis... 19007202
KiSS-1 receptor EC50 = 0.96 nM 9.02 Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increas... 27589480
KiSS-1 receptor EC50 = 0.96 nM 9.02 Agonist activity at human KISS1R transfected in CHO cells assessed as intracellu... 24918545
KiSS-1 receptor Ki = 1.3 nM 8.89 Displacement of [125]metastin from metastin receptor 17266198
KiSS-1 receptor EC50 = 4.2 nM 8.38 Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase ... 27589480
KiSS-1 receptor EC50 = 4.2 nM 8.38 Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellula... 24918545
Neuropeptide FF receptor 1 IC50 = 4.7 nM 8.33 Displacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR1 after 2 hrs 24900254
KiSS-1 receptor EC50 = 17.3 nM 7.76 Activity at metastin receptor expressed in HEK293 cells by measuring calcium rel... 17266198

Literature References

PubMed DOI Target Context # Activities
27589480 10.1021/acs.jmedchem.6b00379 ADMET 8
30598349 10.1016/j.bmcl.2018.12.016 ADMET 7
22975302 10.1016/j.bmcl.2012.08.069 Serum 5
27589480 10.1021/acs.jmedchem.6b00379 Rattus norvegicus 4
24918545 10.1021/jm5005489 KiSS-1 receptor 4
22995619 10.1016/j.bmcl.2012.08.087 Serum 4
22975302 10.1016/j.bmcl.2012.08.069 KiSS-1 receptor 3
24047141 10.1021/jm401056w KiSS-1 receptor 3
24900254 10.1021/ml1002053 Unchecked 3
24900254 10.1021/ml1002053 Neuropeptide FF receptor 1 3
19007202 10.1021/jm800930w KiSS-1 receptor 3
17266198 10.1021/jm0609824 KiSS-1 receptor 2
22995619 10.1016/j.bmcl.2012.08.087 KiSS-1 receptor 2
34008968 10.1021/acs.jmedchem.1c00256 Unchecked 2
24900254 10.1021/ml1002053 Neuropeptide FF receptor 2 2
27589480 10.1021/acs.jmedchem.6b00379 KiSS-1 receptor 2
24900254 10.1021/ml1002053 Rattus norvegicus 1
22975302 10.1016/j.bmcl.2012.08.069 Plasma 1
22995619 10.1016/j.bmcl.2012.08.087 No relevant target 1
24900254 10.1021/ml1002053 KiSS-1 receptor 1

Data from ChEMBL 36 via Core Engine