Target Information

Target General Information

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Target ID

T81905 (Former ID: TTDS00085)

Target Name

Histamine receptor (HR)

Gene Name

NO-GeName

Target Type

Successful target

[1]

Disease

[+] 2 Target-related Diseases

Asthma [ICD-11: CA23]

Diagnostic imaging [ICD-11: N.A.]

BioChemical Class

GPCR rhodopsin

UniProt ID

NOUNIPROTAC

Drugs and Modes of Action

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Approved Drug(s)

[+] 2 Approved Drugs

Histamine Phosphate

Drug Info

Approved

Diagnostic imaging

[2]

Repirinast

Drug Info

Approved

Asthma

[3]

Clinical Trial Drug(s)

[+] 5 Clinical Trial Drugs

Levomequitazine

Drug Info

Phase 3

Seasonal allergic rhinitis

[4]

ETS-6218

Drug Info

Phase 2

Fibromyalgia

[5]

ETX-9101

Drug Info

Phase 2

Asthma

[6]

LCB-2183

Drug Info

Phase 2

Asthma

[7]

Votucalis

Drug Info

Phase 2

Allergic rhinitis

[8]

Discontinued Drug(s)

[+] 5 Discontinued Drugs

OX-NLA

Drug Info

Discontinued in Phase 3

Allergic rhinitis

[9]

CP-118

Drug Info

Discontinued in Phase 2

Allergic rhinitis

[10]

Tesmilifene

Drug Info

Discontinued in Phase 2

Breast cancer

[11]

KF-15766

Drug Info

Terminated

Allergy

[12]

REV-598

Drug Info

Terminated

Carcinoid syndrome

[13]

Mode of Action

[+] 3 Modes of Action

Modulator

[+] 7 Modulator drugs

Histamine Phosphate

Drug Info

[14]

Repirinast

Drug Info

[1], [3]

ETS-6218

Drug Info

[16]

ETX-9101

Drug Info

[16]

LCB-2183

Drug Info

[17]

Tesmilifene

Drug Info

[21]

KF-15766

Drug Info

[22]

Antagonist

[+] 4 Antagonist drugs

Levomequitazine

Drug Info

[15]

Votucalis

Drug Info

[18]

OX-NLA

Drug Info

[19]

CP-118

Drug Info

[20]

Inhibitor

[+] 1 Inhibitor drugs

REV-598

Drug Info

[23]

Drug Property Profile of Target

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(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five

Target Poor or Non Binders

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Target Poor or Non Binders

Target Poor or Non Binders Info

References

Top

REF 1

Mechanism of action of MY-1250, an active metabolite of Repirinast, in inhibiting histamine release from rat mast cells. Br J Pharmacol. 1992 Mar;105(3):587-90.

REF 2

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 000734.

REF 3

Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

REF 4

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800034359)

REF 5

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031879)

REF 6

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800030000)

REF 7

LCB 2183 inhibits tracheal hyperreactivity and pulmonary inflammation in mouse airways. Eur J Pharmacol. 1995 Aug 25;282(1-3):103-9.

REF 8

ClinicalTrials.gov (NCT00353964) Safety and Efficacy Study of rEV131 in the Treatment of Ocular Inflammation After Cataract Surgery. U.S. National Institutes of Health.

REF 9

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020184)

REF 10

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025139)

REF 11

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005041)

REF 12

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005087)

REF 13

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016819)

REF 14

Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.

REF 15

Oxidation of histamine H1 antagonist mequitazine is catalyzed by cytochrome P450 2D6 in human liver microsomes. J Pharmacol Exp Ther. 1998 Feb;284(2):437-42.

REF 16

Clinical pipeline report, company report or official report of e-Therapeutics.

REF 17

LCB 2183 inhibits the inflammation associated with oxazolone-induced contact sensitivity. Int J Immunopharmacol. 1994 Aug;16(8):675-83.

REF 18

CA patent application no. 520580, Histamine binding compounds for treatment method for disease conditions mediated by neutrophils.

REF 19

Clinical pipeline report, company report or official report of Orexo.

REF 20

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025139)

REF 21

Effects of tesmilifene, a substrate of CYP3A and an inhibitor of P-glycoprotein, on the pharmacokinetics of intravenous and oral docetaxel in rats. J Pharm Pharmacol. 2010 Aug;62(8):1084-8.

REF 22

Mutational analysis of the antagonist-binding site of the histamine H(1) receptor. J Biol Chem. 1999 Oct 15;274(42):29994-30000.

REF 23

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016819)

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