Ki Summary

Reaction Details

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Target

Histamine H1 receptor

Ligand

BDBM50002087

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_745951 (CHEMBL1775250)

IC50

1±n/a nM

Citation

Kubota, K; Kurebayashi, H; Miyachi, H; Tobe, M; Onishi, M; Isobe, Y Synthesis and structure-activity relationship of tricyclic carboxylic acids as novel anti-histamines. Bioorg Med Chem19:3005-21 (2011) [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

BDBM50002087

n/a

Name

BDBM50002087

Synonyms:

4-(1-Methyl-piperidin-4-ylidene)-4,9-dihydro-1-thia-benzo[f]azulen-10-one(Ketotifen hydrogen malate) | 4-(1-Methyl-piperidin-4-ylidene)-4,9-dihydro-1-thia-benzo[f]azulen-10-one(Ketotifen) | 4-(1-methyl-piperidin-4-ylidene)-4,9-dihydro-1-thia-benzo[f]azulen-10-one | CHEMBL534 | KETOTIFEN | Zaditor

Type

Small organic molecule

Emp. Form.

C19H19NOS

Mol. Mass.

309.425

SMILES

[#6]-[#7]-1-[#6]-[#6]\[#6](-[#6]-[#6]-1)=[#6]-1\c2ccsc2-[#6](=O)-[#6]-c2ccccc-12

Structure