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Compound Detail

CHEMBL4097878

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CSCC[C@H](NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1CCC[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)[C@H]1CCC[C@@H]1N)C(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CNC[C@@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H]1CCC[C@@H]1C(N)=O)C(C)C)C(C)C

Basic Information

ChEMBL ID CHEMBL4097878
Phase Preclinical
Structure Type MOL
InChI Key HOFYCTUSZAVSDG-MTKKRELOSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
5
Publications
0
Known Names

Molecular Properties

4128.0
MW (Da)

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C188H309N61O42S
MW 4127.99

Activity Summary

EC50 1 meas. best 9.32

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Parathyroid hormone/parathyroid hormone-related peptide receptor
CHEMBL1793
EC50 9.32 9.32 0.5 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 4.0 hr Sus scrofa
T1/2 0.5167 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29064243 10.1021/acs.jmedchem.7b00876 Parathyroid hormone/parathyroid hormone-related peptide receptor 8
29064243 10.1021/acs.jmedchem.7b00876 Unchecked 2
29064243 10.1021/acs.jmedchem.7b00876 Mus musculus 2
29064243 10.1021/acs.jmedchem.7b00876 Blood 1
29064243 10.1021/acs.jmedchem.7b00876 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine