JNJ-39758979

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C11H19N5
Molecular Weight	221.3021
Optical Activity	( - )
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

CC(C)C1=CC(=NC(N)=N1)N2CC[C@@H](N)C2

InChI

InChIKey=COOGVHJHSCBOQT-MRVPVSSYSA-N

InChI=1S/C11H19N5/c1-7(2)9-5-10(15-11(13)14-9)16-4-3-8(12)6-16/h5,7-8H,3-4,6,12H2,1-2H3,(H2,13,14,15)/t8-/m1/s1

HIDE SMILES / InChI

Molecular Formula	C11H19N5
Molecular Weight	221.3021
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

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

Description

JNJ-39758979 is a histamine H4 receptor antagonist which clinical development for asthma and atopic dermatitis was halted during phase II because of the observation of idiosyncratic drug-induced agranulocytosis in two subjects.

Originator

Approval Year

Targets

Targets

Primary Target	Pharmacology	Condition	Potency
Histamine H4 receptor 20	Antagonist 2,778		12.5 nM [Ki]

PubMed

Show entries

Title	Date	PubMed
The histamine H₄ receptor antagonist, JNJ 39758979, is effective in reducing histamine-induced pruritus in a randomized clinical study in healthy subjects.	2014 Jul	24817035
Discovery and SAR of 6-alkyl-2,4-diaminopyrimidines as histamine H₄ receptor antagonists.	2014 Mar 27	24495018
International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.	2015 Jul	26084539