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Target
Substance-P receptor
Ligand
BDBM50002382
Substrate
n/a
Meas. Tech.
ChEBML_208658
IC50
1200±n/a nM
Citation
 Venepalli, BR; Aimone, LD; Appell, KC; Bell, MR; Dority, JA; Goswami, R; Hall, PL; Kumar, V; Lawrence, KB; Logan, ME Synthesis and substance P receptor binding activity of androstano[3,2-b]pyrimido[1,2-a]benzimidazoles. J Med Chem 35:374-8 (1992) [PubMed]  Article 
Target
Name:
Substance-P receptor
Synonyms:
NK-1 receptor | NK-1R | NK1 Receptor | NK1R_RAT | Neurokinin 1 receptor | Neurokinin NK1 | SPR | Substance-P receptor | Tac1r | Tachykinin receptor 1 | Tacr1
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
46371.54
Organism:
Rattus norvegicus (rat)
Description:
Competition binding assays were carried out using membrane preparations from transfected CHO cells that constitutively expressed the rat NK1 receptor.
Residue:
407
Sequence:
MDNVLPMDSDLFPNISTNTSESNQFVQPTWQIVLWAAAYTVIVVTSVVGNVVVIWIILAHKRMRTVTNYFLVNLAFAEACMAAFNTVVNFTYAVHNVWYYGLFYCKFHNFFPIAALFASIYSMTAVAFDRYMAIIHPLQPRLSATATKVVIFVIWVLALLLAFPQGYYSTTETMPSRVVCMIEWPEHPNRTYEKAYHICVTVLIYFLPLLVIGYAYTVVGITLWASEIPGDSSDRYHEQVSAKRKVVKMMIVVVCTFAICWLPFHVFFLLPYINPDLYLKKFIQQVYLASMWLAMSSTMYNPIIYCCLNDRFRLGFKHAFRCCPFISAGDYEGLEMKSTRYLQTQSSVYKVSRLETTISTVVGAHEEEPEEGPKATPSSLDLTSNGSSRSNSKTMTESSSFYSNMLA
  
Inhibitor
Name:
BDBM50002382
Synonyms:
1-(1-ethynyl)-1-hydroxy-16a,18a-dimethyl-(1R,5aS,16aS,18aS)-1,2,3,3a,3b,4,5,5a,6,13,16,16a,16b,17,18,18a-hexadecahydrocyclopenta[5,6]naphtho[1,2-g]quinazolino[2,3-b]quinazolin-13-one(0.5MH2O) | CHEMBL3138259
Type:
Small organic molecule
Emp. Form.:
C30H33N3O2
Mol. Mass.:
467.6019
SMILES:
[H][C@@]12CC[C@@](O)(C#C)[C@@]1(C)CC[C@@]1([H])[C@@]2([H])CC[C@@]2([H])Cc3nc4nc5ccccc5c(=O)n4cc3C[C@]12C
Structure:
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