Ki Summary BindingDB logo
Reaction Details
Report a problem with these data
TargetHistamine H3 Receptor
LigandJNJ 7777120
Substrate/Competitor[3H]N-alpha-methyl histamine
Meas. Tech.Radioligand Binding Assay
pH7.4±n/a
Temperature298.15±n/a K
Ki 1318±260 nM
Citation Altenbach, RJAdair, RMBettencourt, BMBlack, LAFix-Stenzel, SRGopalakrishnan, SMHsieh, GCLiu, HMarsh, KCMcPherson, MJMilicic, IMiller, TRVortherms, TAWarrior, UWetter, JMWishart, NWitte, DGHonore, PEsbenshade, TAHancock, AABrioni, JDCowart, MD Structure-activity studies on a series of a 2-aminopyrimidine-containing histamine H4 receptor ligands.J Med Chem.51:6571-80(2008)[PubMed]
More Info. Get all data from this article ,   Solution Info ,  Assay Method
Histamine H3 Receptor
NameHistamine H3 Receptor
SynonymsHH3R
TypeG Protein-Coupled Receptor (GPCR)
Mol. Mass.48588
OrganismRattus norvegicus (rat)
DescriptionRadioligand binding assays were using rat cortical membranes.
Residue445
Sequence
MERAPPDGLMNASGTLAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFV
ADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCAS
SVFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMALVWVLAFLLYGPAILSWEYLSGG
SSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGGREAG
PEPPPDAQPSPPPAPPSCWGCWPKGHGEAMPLHRYGVGEAGPGVEAGEAALGGGSGGGAA
ASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSITQRFRLSRDKKVAKSL
AIIVSIFGLCWAPYTLLMIIRAACHGRCIPDYWYETSFWLLWANSAVNPVLYPLCHYSFR
RAFTKLLCPQKLKVQPHGSLEQCWK
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
JNJ 7777120
NameJNJ 7777120
Synonyms:5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-indole
TypeSmall organic molecule
Emp. Form.C14H16ClN3O
Mol. Mass.277.749
SMILESCN1CCN(CC1)C(=O)c1cc2cc(Cl)ccc2[nH]1
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
[3H]N-alpha-methyl histamine
Name[3H]N-alpha-methyl histamine
Synonyms:N-alpha-methylhistamine | N-methylhistamine | [2-(1H-imidazol-5-yl)ethyl](methyl)amine
Typeradiolabeled ligand
Emp. Form.C6H11N3
Mol. Mass.125.1716
SMILESCNCCc1cnc[nH]1
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: