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Compound Detail

CHEMBL262747

ACYLINE
🧪 Phase II
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🧪 Phase II
CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1

Basic Information

ChEMBL ID CHEMBL262747
Name ACYLINE
Phase Phase II
Structure Type MOL
InChI Key ZWNUQDJANZGVFO-YHSALVGYSA-N

Known Names

Acyline MER-104
2
Targets
6
Activities
2
Assay Types
0
PK Parameters
9
Publications
2
Known Names
1
Indications
1
Mechanisms

Molecular Properties

1533.2
MW (Da)

Drug Information

Molecule Type Protein
Chirality Single Enantiomer

Flags

Natural Product

Extended Properties

Molecular Formula C80H102ClN15O14
MW 1533.24

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Gonadotropin-releasing hormone receptor antagonist ANTAGONIST Gonadotropin-releasing hormone receptor

Indications

Hypogonadism

Activity Summary

IC50 5 meas. best 9.28
Kd 1 meas. best 8.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Gonadotropin-releasing hormone receptor
CHEMBL1855
IC50 9.28 8.9425 0.5 4
Gonadotropin-releasing hormone receptor
CHEMBL3066
IC50 8.82 8.82 1.5 1
Gonadotropin-releasing hormone receptor
CHEMBL1855
Kd 8.6 8.6 2.5 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11462984 10.1021/jm0003900 Rattus norvegicus 5
17402723 10.1021/jm0613931 Gonadotropin-releasing hormone receptor 3
11462984 10.1021/jm0003900 Gonadotropin-releasing hormone receptor 2
16759096 10.1021/jm060240a Gonadotropin-releasing hormone receptor 2
16759096 10.1021/jm060240a Mast cell 1
16759096 10.1021/jm060240a Rattus norvegicus 1
17402723 10.1021/jm0613931 Unchecked 1
17402723 10.1021/jm0613931 Rattus norvegicus 1
17402723 10.1021/jm0613931 No relevant target 1

Data from ChEMBL 36 via Core Engine