Reaction Details Report a problem with these data
Target
Histamine H1 receptor
Ligand
BDBM22566
Substrate
BDBM22567
Meas. Tech.
Radioligand Binding Assay
pH
7.5±n/a
Temperature
298.15±n/a K
Ki
>10000±n/a nM
Citation
 Thurmond, RL; Desai, PJ; Dunford, PJ; Fung-Leung, WP; Hofstra, CL; Jiang, W; Nguyen, S; Riley, JP; Sun, S; Williams, KN; Edwards, JP; Karlsson, L A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties. J Pharmacol Exp Ther 309:404-13 (2004) [PubMed]  Article 
Target
Name:
Histamine H1 receptor
Synonyms:
Bphs | HRH1_MOUSE | Hrh1
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
55705.87
Organism:
Mus musculus (mouse)
Description:
n/a
Residue:
488
Sequence:
MSLPNTSSASEDKMCEGNRTAMASPQLLPLVVVLSSISLVTVGLNLLVLYAVRSERKLHTVGNLYIVSLSVADLIVGAVVMPMNILYLIMTKWSLGRPLCLFWLSMDYVASTASIFSVFILCIDRYRSVQQPLRYLRYRTKTRASATILGAWFLSFLWVIPILGWHHFTPLAPELREDKCETDFYNVTWFKIMTAIINFYLPTLLMLWFYVKIYKAVRRHCQHRQLTNGSLPTFLEIKLRSEDAKEGAKKPGKESPWGVQKRPSRDPTGGLDQKSTSEDPKVTSPTVFSQEGERETVTRPCFRLDVMQTQPVPEGDARGSKANDQTLSQPKMDEQSLSTCRRISETSEDQTLVDRQSFSRTTDSDTSIEPGLGKVKARSRSNSGLDYIKVTWKRLRSHSRQYVSGLHLNRERKAAKQLGCIMAAFILCWIPYFIFFMVIAFCNSCCSEPVHMFTIWLGYINSTLNPLIYPLCNENFKKTFKKILHIRS
  
Inhibitor
Name:
BDBM22566
Synonyms:
5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-indole | CHEMBL129198 | JNJ 7777120
Type:
Small organic molecule
Emp. Form.:
C14H16ClN3O
Mol. Mass.:
277.749
SMILES:
CN1CCN(CC1)C(=O)c1cc2cc(Cl)ccc2[nH]1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM22567
Synonyms:
3H]pyrilamine | CHEMBL511 | Dorantamin | Mepyramine | N-(4-methoxybenzyl)-N ,N -dimethyl-N-pyridin-2-ylethane-1,2-diamine | N-[2-(dimethylamino)ethyl]-N-[(4-methoxyphenyl)methyl]pyridin-2-amine | PYRILAMINE | Pyranisamine | [3H]mepyramine | [3H]pyrilamine
Type:
radiolabeled ligand
Emp. Form.:
C17H23N3O
Mol. Mass.:
285.384
SMILES:
COc1ccc(CN(CCN(C)C)c2ccccn2)cc1
Structure:
Search PDB for entries with ligand similarity: