Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DML51D0)

• Drug Name: UCL-2000; butabindide Drug Info

Indication

Disease Entry	ICD 11	Status	REF
Obesity	5B81	Discontinued in Phase 1	[1]

• Cross-matching ID: TTD Drug ID: DML51D0

Molecule-Related Drug Atlas

Drug(s) Targeting Cholecystokinin receptor type A (CCKAR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Dexloxiglumide	DM52HUD	Pancreatic malfunction	DC30-DC3Z	Phase 2	[3]
proglumide	DM4MF9V	Influenza virus infection	1E30-1E32	Phase 2	[4]
Lintitript	DMS5X94	Obesity	5B81	Discontinued in Phase 2	[5]
Tarazepide	DMX6ZYE	Gastrointestinal disease	DE2Z	Discontinued in Phase 2	[6]
GI 181771	DMIUFS4	Obesity	5B81	Discontinued in Phase 2	[7]
Pranazepide	DMP43IR	Pancreatic malfunction	DC30-DC3Z	Discontinued in Phase 2	[8]
CE-326597	DMXO49B	Obesity	5B81	Discontinued in Phase 2	[9]
SSR-125180	DMSOBW2	Obesity	5B81	Discontinued in Phase 1	[10]
T-0632	DML4M5K	Pancreatic malfunction	DC30-DC3Z	Discontinued in Phase 1	[11]
SR-146131	DML7KCO	Obesity	5B81	Discontinued in Phase 1	[12]

Drug(s) Targeting Tripeptidyl-peptidase II (TPP2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(2S)-aminobutyryl-L-proline-(2S)-methylbutylamide	DMEWU6Z	Discovery agent	N.A.	Investigative	[13]
L-valyl-L-prolinamide	DMH7TNA	Discovery agent	N.A.	Investigative	[13]
(2S)-aminobutyryl-L-proline n-butylamide	DM12Q9O	Discovery agent	N.A.	Investigative	[13]
L-norvalyl-L-prolinamide	DMIXFGC	Discovery agent	N.A.	Investigative	[13]
L-valyl-L-proline benzylamide	DMQZ13A	Discovery agent	N.A.	Investigative	[13]
(2S)-aminobutyryl-L-prolinamide	DMG0QKL	Discovery agent	N.A.	Investigative	[13]
peptide 4	DM45RTZ	Discovery agent	N.A.	Investigative	[14]
example 8 [WO1999033801A1]	DMFSHXW	Discovery agent	N.A.	Investigative	[15]
(2S)-aminobutyryl-(R)-pipecolinic acid amide	DMWQK86	Discovery agent	N.A.	Investigative	[13]
L-norleucyl-L-prolinamide	DM7V30L	Discovery agent	N.A.	Investigative	[13]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Cholecystokinin receptor type A (CCKAR)	TTCG0AL	CCKAR_HUMAN	Agonist	[2]
Tripeptidyl-peptidase II (TPP2)	TTQ7R2V	TPP2_HUMAN	Inhibitor	[2]

References

• [1] Clinical pipeline report, company report or official report of University College London.
• [2] Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.
• [3] Full agonists of CCK8 containing a nonhydrolyzable sulfated tyrosine residue. J Med Chem. 1989 Feb;32(2):445-9.
• [4] Pharmacological properties of lorglumide as a member of a new class of cholecystokinin antagonists. Arzneimittelforschung. 1987 Nov;37(11):1265-8.
• [5] A cholecystokinin-1 receptor agonist (CCK-8) mediates increased permeability of brain barriers to leptin. Br J Pharmacol. 2008 Jul;154(5):1009-15.
• [6] Melatonin as modulator of pancreatic enzyme secretion and pancreatoprotector. J Physiol Pharmacol. 2007 Dec;58 Suppl 6:65-80.
• [7] Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2003 Jul-Aug;25(6):483-506.
• [8] Dual CCK-A and -B receptor antagonists (I) C9-methyl-1,4-benzodiazepines, Bioorg. Med. Chem. Lett. 7(2):169-174 (1997).
• [9] Obesity Pharmacotherapy: Current Perspectives and Future Directions. Curr Cardiol Rev. 2013 February; 9(1): 33-54.
• [10] US patent application no. 8,748,419, Antagonists.
• [11] Effect of T-0632, a cholecystokininA receptor antagonist, on experimental acute pancreatitis. Jpn J Pharmacol. 1997 Feb;73(2):105-12.
• [12] SR146131: a new potent, orally active, and selective nonpeptide cholecystokinin subtype 1 receptor agonist. I. In vitro studies. J Pharmacol Exp Ther. 1999 May;289(2):742-51.
• [13] Inhibitors of tripeptidyl peptidase II. 3. Derivation of butabindide by successive structure optimizations leading to a potential general approach ... J Med Chem. 2005 Nov 17;48(23):7333-42.
• [14] Use of lantibiotic synthetases for the preparation of bioactive constrained peptides. Bioorg Med Chem Lett. 2008 May 15;18(10):3025-8.
• [15] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2423).