General
Preferred name
MK-0893
Synonyms
MK 0893 ()
Mk0893 ()
P&D ID
PD051655
CAS
870823-12-4
Tags
available
drug candidate
Drug Status
investigational
Max Phase
2.0
Drug indication
type 2 diabetes mellitus
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION MK-0893 is reported as a potent, reversible and competitive antagonist of the glucagon receptor, with anti-type II diabetes potential . X-ray crystallography shows that MK-0893 in fact binds to an allosteric site outside the seven transmembrane bundle . (GtoPdb)
DESCRIPTION MK 0893 is a potent and selective glucagon receptor antagonist with an IC50 of 6.6 nM.
DESCRIPTION MK-0893 is a potent, selective glucagon receptor antagonist with high binding affinity with IC(50) of 6.6 nM and functional cAMP activity with IC(50) of 15.7 nM. It is selective for glucagon receptor relative to other family B GPCRs and is > 200 fold selectivity for GIPR, PAC1, GLP-1R, VPAC1 and VPAC2. It blunted glucagon-induced glucose elevation in hGCGR mice and rhesus monkeys. It may be a potential oral treatment for type 2 diabetes. It was selected for further preclinical and clinical evaluations. (BOC Sciences Bioactive Compounds)
Compound Sets
9
BOC Sciences Bioactive Compounds
mk-0893-cas-870823-12-4-221506
ChEMBL Drugs
CHEMBL1933349
Drug Repurposing Hub
DrugBank
DB12044
Guide to Pharmacology
9135
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL1933349
MedChem Express Bioactive Compound Library
HY-50663
ReFrame library
ZINC Tool Compounds
ZINC000068250425
External IDs
26
Properties
(calculated by RDKit )
Molecular Weight
587.14
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
2
Rotatable Bonds
9
Ring Count
5
Aromatic Ring Count
5
cLogP
7.5
TPSA
93.45
Fraction CSP3
0.16
Chiral centers
1.0
Largest ring
6.0
QED
0.19
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
GCGR
MOA
glucagon receptor antagonist
Pathway
GPCR/G protein
Solubility
10 mM in DMSO
Source data