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Compound Detail

CHEMBL438926

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CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CC(N)=O)NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)CNC(=O)CNC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)C(C)C)[C@@H](C)O)C(C)C)[C@@H](C)O)C(C)C)C(N)=O

Basic Information

ChEMBL ID CHEMBL438926
Phase Preclinical
Structure Type BOTH
InChI Key PUBCCFNQJQKCNC-XKNFJVFFSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

2859.4
MW (Da)

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C130H204N38O31S2
MW 2859.43

Activity Summary

EC50 3 meas. best 7.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Gastrin-releasing peptide receptor
CHEMBL4959
EC50 7.47 7.47 34.0 1
Neuromedin-B receptor
CHEMBL3636
EC50 5.5 5.5 3200.0 1
Bombesin receptor subtype-3
CHEMBL4080
EC50 5.19 5.19 6400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12723954 10.1021/jm0210921 Neuromedin-B receptor 1
12723954 10.1021/jm0210921 Gastrin-releasing peptide receptor 1
12723954 10.1021/jm0210921 Bombesin receptor subtype-3 1

Data from ChEMBL 36 via Core Engine