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Compound Detail

CHEMBL4093140

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CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)CN[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C

Basic Information

ChEMBL ID CHEMBL4093140
Phase Preclinical
Structure Type MOL
InChI Key RDCIPOBDQMOUKD-LXJGJVCSSA-N
4
Targets
8
Activities
2
Assay Types
1
PK Parameters
6
Publications
0
Known Names

Molecular Properties

1632.9
MW (Da)

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C78H113N21O18
MW 1632.89

Activity Summary

EC50 4 meas. best 11.0
IC50 4 meas. best 11.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melanocyte-stimulating hormone receptor
CHEMBL3795
EC50 11.0 11.0 0.0 1
Melanocyte-stimulating hormone receptor
CHEMBL3795
IC50 11.0 11.0 0.0 1
Melanocortin receptor 4
CHEMBL259
EC50 9.7 9.7 0.2 1
Melanocortin receptor 4
CHEMBL259
IC50 9.4 9.4 0.4 1
Melanocortin receptor 3
CHEMBL4644
EC50 9.1 9.1 0.8 1
Melanocortin receptor 5
CHEMBL4608
EC50 9.0 9.0 1.0 1
Melanocortin receptor 5
CHEMBL4608
IC50 8.66 8.66 2.2 1
Melanocortin receptor 3
CHEMBL4644
IC50 8.48 8.48 3.3 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.5 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29094944 10.1021/acs.jmedchem.7b01295 Melanocyte-stimulating hormone receptor 4
29094944 10.1021/acs.jmedchem.7b01295 Melanocortin receptor 3 4
29094944 10.1021/acs.jmedchem.7b01295 Melanocortin receptor 4 4
29094944 10.1021/acs.jmedchem.7b01295 Melanocortin receptor 5 4
29094944 10.1021/acs.jmedchem.7b01295 Anolis carolinensis 3
29094944 10.1021/acs.jmedchem.7b01295 Serum 1

Data from ChEMBL 36 via Core Engine