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Compound Detail

CHEMBL1007

GONADORELIN
💊 Approved Drug
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💊 Approved Drug
CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL1007
Name GONADORELIN
Phase Approved
Structure Type BOTH
InChI Key XLXSAKCOAKORKW-AQJXLSMYSA-N
Therapeutic ✓ Yes

Known Names

Fertiral lh-rh Gonadorelin Gonadorelin decapeptide Gonadorelina Gonadoreline Gonadotropin-releasing hormone Relefact lh-rh
3
Targets
6
Activities
2
Assay Types
3
PK Parameters
17
Publications
7
Known Names
4
Indications

Molecular Properties

1182.3
MW (Da)

Drug Information

Molecule Type Protein
First Approval 1982
Availability Discontinued
Chirality Single Enantiomer

Routes of Administration

Parenteral

Flags

Natural Product
USAN Stem -relin
USAN Year 1975

Extended Properties

Molecular Formula C55H75N17O13
MW 1182.31

Indications

Osteoporosis Prostatic Neoplasms, Castration-Resistant Breast Neoplasms Cocaine-Related Disorders

ATC Classification

H01CA01
gonadorelin
Level 1: SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS
Level 2: PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES
V04CM01
gonadorelin
Level 1: VARIOUS
Level 2: DIAGNOSTIC AGENTS

Activity Summary

IC50 4 meas. best 8.7
Ki 2 meas. best 8.9

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Lutropin-choriogonadotropic hormone receptor
CHEMBL2456
 Ki 8.9 8.9 1.3 1
Gonadotropin-releasing hormone receptor
CHEMBL3066
 IC50 8.7 8.3567 2.0 3
Gonadotropin-releasing hormone receptor
CHEMBL1855
 IC50 8.0 8.0 10.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.05 hr Homo sapiens
T1/2 0.5433 hr Homo sapiens
T1/2 2.63 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Lutropin-choriogonadotropic hormone receptor Ki = 1.259 nM 8.9 In vitro binding affinity for Luteinizing hormone releasing hormone receptor fro... 2552116
Gonadotropin-releasing hormone receptor IC50 = 2.0 nM 8.7 Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-... 10956191
Gonadotropin-releasing hormone receptor IC50 = 6.0 nM 8.22 The compound was tested for the concentration to inhibit 50% of [125 I]leuprorel... 9784092
Gonadotropin-releasing hormone receptor IC50 = 7.0 nM 8.15 The compound was tested for the concentration to inhibit 50% of [125 I]leuprorel... 9784092
Gonadotropin-releasing hormone receptor IC50 = 10.0 nM 8.0 The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprore... 9784092

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL3885741 Gonadotropin-releasing hormone receptor 4
1255667 10.1021/jm00225a018 Rattus norvegicus 4
9784092 10.1021/jm9803673 Gonadotropin-releasing hormone receptor 3
3279211 10.1021/jm00398a030 Rattus norvegicus 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
- 10.6019/CHEMBL4651402 SARS-CoV-2 2
342693 10.1021/jm00201a008 Rattus norvegicus 2
23712085 10.1016/j.bmc.2013.04.068 Caco-2 2
2552116 10.1021/jm00130a019 Lutropin-choriogonadotropic hormone receptor 2
7009870 10.1021/jm00134a021 Rattus norvegicus 2
23127987 10.1016/j.ejmech.2012.09.043 ADMET 1
23712085 10.1016/j.bmc.2013.04.068 Plasma 1
23127987 10.1016/j.ejmech.2012.09.043 Unchecked 1
10956191 10.1021/jm990433g Gonadotropin-releasing hormone receptor 1
8381183 10.1021/jm00055a007 Rattus norvegicus 1
- 10.1039/C5MD00259A Plasma 1
8381183 10.1021/jm00055a007 Gonadotropin-releasing hormone receptor 1

Data from ChEMBL 36 via Core Engine