PF-5190457

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NCATS

Investigational

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C29H32N6OS
Molecular Weight	512.669
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure of PF-5190457

Structure Search

SMILES

CC1=CN2C=C(CC(=O)N3CCC4(CN(C4)[C@@H]5CCC6=CC(=CC=C56)C7=NC=NC(C)=C7)CC3)N=C2S1

InChI

InChIKey=ZIUDADZJCKGWKR-AREMUKBSSA-N

InChI=1S/C29H32N6OS/c1-19-11-25(31-18-30-19)22-3-5-24-21(12-22)4-6-26(24)35-16-29(17-35)7-9-33(10-8-29)27(36)13-23-15-34-14-20(2)37-28(34)32-23/h3,5,11-12,14-15,18,26H,4,6-10,13,16-17H2,1-2H3/t26-/m1/s1

HIDE SMILES / InChI

Molecular Formula	C29H32N6OS
Molecular Weight	512.669
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

Approval Year

Targets

Targets

Primary Target	Pharmacology	Condition	Potency
Ghrelin receptor 15 Target ID: CHEMBL4616 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24900864	Inverse Agonist 80		8.36 null [pKi]

Patents

Patents

Substance Class	Chemical Created by `admin` on `Sat Dec 16 01:39:34 UTC 2023` Edited by `admin` on `Sat Dec 16 01:39:34 UTC 2023`
Record UNII	FF33NL9U5G
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

PF-5190457

Code

English

ETHANONE, 1-(2-((1R)-2,3-DIHYDRO-5-(6-METHYL-4-PYRIMIDINYL)-1H-INDEN-1-YL)-2,7-DIAZASPIRO(3.5)NON-7-YL)-2-(2-METHYLIMIDAZO(2,1-B)THIAZOL-6-YL)-

Systematic Name

English

PF-05190457

Common Name

English

Code System Code Type Description

CAS

1334782-79-4

Created by admin on Sat Dec 16 01:39:34 UTC 2023 , Edited by admin on Sat Dec 16 01:39:34 UTC 2023

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DRUG BANK

DB14870

Created by admin on Sat Dec 16 01:39:34 UTC 2023 , Edited by admin on Sat Dec 16 01:39:34 UTC 2023

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PUBCHEM

58438464

Created by admin on Sat Dec 16 01:39:34 UTC 2023 , Edited by admin on Sat Dec 16 01:39:34 UTC 2023

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MANUFACTURER PRODUCT INFORMATION

PF-05190457

Created by admin on Sat Dec 16 01:39:34 UTC 2023 , Edited by admin on Sat Dec 16 01:39:34 UTC 2023

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MedKoo CAT NO.: 522485, CAS NO.: 1334782-79-4Description: PF-5190457 is an orally available, potent and selective ghrelin receptor inverse agonist. PF-5190457 potently increases insulin secretion in glucose-stimulated human islets. PF-5190457 has a superior balance of ghrelin receptor pharmacology and off-target selectivity. On the basis of its promising pharmacological and safety profile, PF-5190457 was advanced to human clinical trials. (last updated: 11/10/2015).

FDA UNII

FF33NL9U5G

Created by admin on Sat Dec 16 01:39:34 UTC 2023 , Edited by admin on Sat Dec 16 01:39:34 UTC 2023

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SMS_ID

300000041357

Created by admin on Sat Dec 16 01:39:34 UTC 2023 , Edited by admin on Sat Dec 16 01:39:34 UTC 2023

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Comments:

Originator: Pfizer; Class: Antihyperglycaemic; Mechanism of Action: Undefined mechanism; Orphan Drug Status: No; On Fast track: No; New Molecular Entity: Yes; Highest Development Phase: No development reported for Type 2 diabetes mellitus; Most Recent Events: 16 Jul 2016 No recent reports of development identified for phase-I development in Type-2-diabetes-mellitus(In volunteers) in Singapore (PO), 16 Jul 2016 No recent reports of development identified for phase-I development in Type-2-diabetes-mellitus(In volunteers) in Belgium (PO), 18 Apr 2012 Discontinued - Phase-I for Type-2 diabetes mellitus in USA (PO)

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ACTIVE MOIETY

Comments:

Official Title: A Novel Compound for Alcoholism Treatment: A Translational Strategy Purpose: Background: Hormones are naturally occurring chemicals in your body. Ghrelin is a hormone that is mainly produced by the stomach and stimulates appetite. Some studies suggest it may stimulate alcohol craving and use. Drugs have been developed that block ghrelin. Researchers want to know if people can tolerate a particular drug that blocks ghrelin. It will be given at two dose levels, combined with alcohol. Objective: To determine if a drug that may decrease alcohol consumption when given along with alcohol is safe and tolerable.

Amount: