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

PD136450 Drug Info

PD-136450; Cam 1189; PD 136450; CHEMBL341460; CHEMBL3351022; (E)-4-[[(1R)-2-[[(2R)-2-(2-adamantyloxycarbonylamino)-3-(1H-indol-3-yl)-2-methylpropanoyl]amino]-1-phenylethyl]amino]-4-oxobut-2-enoic acid; PD136450; CAM-1189; AC1O5RMN; GTPL867; SCHEMBL6895211; BDBM50230677; BDBM50007439; PD-136,450; 2-Butenoic acid, 4-((2-((3-(1H-indol-3-yl)-2-methyl-1-oxo-2-(((tricyclo(3.3.1.1(3,7))dec-2-yloxy)carbonyl)amino)propyl)amino)-1-phenylethyl)amino)-4-oxo-, (R-(R*,R*))-

Cross-matching ID

PubChem CID

6439414

CAS Number

CAS 139067-52-0

TTD Drug ID

DMD6L82

General Information of Drug (ID: DMD6L82)

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Approved Drug(s)

Clinical Trial Drug(s)

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Drug(s) Targeting Gastrin/cholecystokinin type B receptor (CCKBR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Pentagastrin	DMRCLZB	Diagnostic imaging	N.A.	Approved	[2]
Ceruletide	DM2WE5K	Caerulein stimulated gastric and pancreatic secretion	5A4Y	Approved	[3]
GASTRAZOLE	DMO3ITF	Duodenal ulcer	DA63	Phase 3	[4]
Dexloxiglumide	DM52HUD	Pancreatic malfunction	DC30-DC3Z	Phase 2	[5]
Spiroglumide	DM7NJWY	Stomach disease	DA43-DA4Y	Phase 2	[6]
TT-223	DMCDMFP	Type-1 diabetes	5A10	Phase 2	[7]
Z 360	DM2M80G	Discovery agent	N.A.	Phase 2	[8]
S-0509	DM4KWEF	Ulcerative colitis	DD71	Phase 2	[9]
YF-476	DM54MAJ	Stomach ulcer	DA60.Z	Phase 2	[10]
Itriglumide	DM5UFRO	Anxiety disorder	6B00-6B0Z	Phase 2	[11]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Gastrin/cholecystokinin type B receptor (CCKBR)	TTVFO0U	GASR_HUMAN	Antagonist	[1]

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References

1	Cholecystokinin type B receptor antagonist PD-136,450 is a partial secretory agonist in the stomach and a full agonist in the pancreas of the rat. Gut. 1994 Feb;35(2):270-4.
2	Functional interactions between endocannabinoid and CCK neurotransmitter systems may be critical for extinction learning. Neuropsychopharmacology. 2009 Jan;34(2):509-21.
3	Comparison of postprandial and ceruletide serum bile acid stimulation in dogs. J Vet Intern Med. 2008 Jul-Aug;22(4):873-8.
4	Gastrazole (JB95008), a novel CCK2/gastrin receptor antagonist, in the treatment of advanced pancreatic cancer: results from two randomised controlled trials. Br J Cancer. 2006 April 24; 94(8): 1107-1115.
5	Synthesis and stereochemical structure-activity relationships of 1,3-dioxoperhydropyrido[1,2-c]pyrimidine derivatives: potent and selective cholecy... J Med Chem. 1997 Oct 10;40(21):3402-7.
6	Effect of dexloxiglumide and spiroglumide, two new CCK-receptor antagonists, on gastric emptying and secretion in the rat: evaluation of their receptor selectivity in vivo. Aliment Pharmacol Ther. 1996 Jun;10(3):411-9.
7	The effect of glucagon-like peptide-1 on energy expenditure and substrate metabolism in humans. Int J Obes Relat Metab Disord. 2000 Mar;24(3):288-98.
8	Z-360, a novel cholecystokinin-2/gastrin receptor antagonist, inhibits gemcitabine-induced expression of the vascular endothelial growth factor gen... Biol Pharm Bull. 2010;33(2):216-22.
9	Selective action of a CCK-B/gastrin receptor antagonist, S-0509, on pentagastrin-, peptone meal- and beer-stimulated gastric acid secretion in dogs. Aliment Pharmacol Ther. 2000 Apr;14(4):479-88.
10	CCK-B receptor antagonist YF476 inhibits pancreatic enzyme secretion at a duodenal level in pigs. Scand J Gastroenterol. 2004 Sep;39(9):886-90.
11	Role of CCK/gastrin receptors in gastrointestinal/metabolic diseases and results of human studies using gastrin/CCK receptor agonists/antagonists in these diseases. Curr Top Med Chem. 2007; 7(12): 1211-1231.