Ki Summary

Reaction Details

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Target

Histamine H1 receptor

Ligand

BDBM50191289

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_556998 (CHEMBL960689)

7.76±n/a nM

Citation

Smits, RA; de Esch, IJ; Zuiderveld, OP; Broeker, J; Sansuk, K; Guaita, E; Coruzzi, G; Adami, M; Haaksma, E; Leurs, R Discovery of quinazolines as histamine H4 receptor inverse agonists using a scaffold hopping approach. J Med Chem51:7855-65 (2008) [PubMed] Article

More Info.:

Get all data from this article, Assay Method

Histamine H1 receptor

Name:

Histamine H1 receptor

Synonyms:

H1R | HH1R | HISTAMINE H1 | HRH1 | HRH1_HUMAN

Type:

G Protein-Coupled Receptor (GPCR)

Mol. Mass.:

55808.72

Organism:

Homo sapiens (Human)

Description:

Cell pellets from SK-N-MC cells transfected with human H1 receptor were used in binding assay.

Residue:

487

Sequence:

MSLPNSSCLLEDKMCEGNKTTMASPQLMPLVVVLSTICLVTVGLNLLVLYAVRSERKLHT
VGNLYIVSLSVADLIVGAVVMPMNILYLLMSKWSLGRPLCLFWLSMDYVASTASIFSVFI
LCIDRYRSVQQPLRYLKYRTKTRASATILGAWFLSFLWVIPILGWNHFMQQTSVRREDKC
ETDFYDVTWFKVMTAIINFYLPTLLMLWFYAKIYKAVRQHCQHRELINRSLPSFSEIKLR
PENPKGDAKKPGKESPWEVLKRKPKDAGGGSVLKSPSQTPKEMKSPVVFSQEDDREVDKL
YCFPLDIVHMQAAAEGSSRDYVAVNRSHGQLKTDEQGLNTHGASEISEDQMLGDSQSFSR
TDSDTTTETAPGKGKLRSGSNTGLDYIKFTWKRLRSHSRQYVSGLHMNRERKAAKQLGFI
MAAFILCWIPYFIFFMVIAFCKNCCNEHLHMFTIWLGYINSTLNPLIYPLCNENFKKTFK
RILHIRS

BDBM50191289

n/a

Name

BDBM50191289

Synonyms:

7-chloro-11-(4-methyl-piperazin-1-yl)-dibenzo[b,f][1,4]oxazepine | 7-chloro-11-(4-methylpiperazin-1-yl)-dibenzo[b,f][1,4]oxazepine | 7-chloro-11-(4-methylpiperazin-1-yl)dibenzo[b,f][1,4]oxazepine | CHEMBL213912 | VUF-6884

Type

Small organic molecule

Emp. Form.

C18H18ClN3O

Mol. Mass.

327.808

SMILES

CN1CCN(CC1)C1=Nc2ccc(Cl)cc2Oc2ccccc12 |t:8|

Structure