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Compound Detail

CHEMBL4086979

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CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O)[C@@H](C)CC)C(=O)O

Basic Information

ChEMBL ID CHEMBL4086979
Phase Preclinical
Structure Type MOL
InChI Key QSTDEEQYDKLIQV-RNTNRNDHSA-N
1
Targets
4
Activities
1
Assay Types
4
PK Parameters
3
Publications
0
Known Names

Molecular Properties

4582.1
MW (Da)

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C203H319N57O64
MW 4582.12

Activity Summary

EC50 4 meas. best 10.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glucagon receptor
CHEMBL4773
EC50 10.6 10.6 0.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 11000.0 ng.hr.mL-1 Mus musculus
Cmax 421.2 nM Mus musculus
T1/2 3.2 hr Mus musculus
Tmax 1.0 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Glucagon receptor EC50 = 0.025 nM 10.6 Agonist activity at mouse glucagon receptor expressed in HEK293 cells assessed a... 28448133

Literature References

PubMed DOI Target Context # Activities
28448133 10.1021/acs.jmedchem.7b00174 Mus musculus 7
28448133 10.1021/acs.jmedchem.7b00174 Glucagon-like peptide 1 receptor 2
28448133 10.1021/acs.jmedchem.7b00174 Glucagon receptor 2

Data from ChEMBL 36 via Core Engine