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Target
5-hydroxytryptamine receptor 1A
Ligand
BDBM29567
Substrate
BDBM21393
Meas. Tech.
Radioligand Binding Assay (Ki)
pH
7.4±n/a
Temperature
310.15±n/a K
Ki
1.3±0.2 nM
Citation
 Paluchowska, MH; Bugno, R; Duszyńska, B; Tatarczyńska, E; Nikiforuk, A; Lenda, T; Chojnacka-Wójcik, E The influence of modifications in imide fragment structure on 5-HT(1A) and 5-HT(7) receptor affinity and in vivo pharmacological properties of some new 1-(m-trifluoromethylphenyl)piperazines. Bioorg Med Chem 15:7116-25 (2007) [PubMed]  Article 
Target
Name:
5-hydroxytryptamine receptor 1A
Synonyms:
5-HT-1A | 5-HT1 | 5-HT1A | 5-Hydroxytryptamine receptor 1A (5-HT1A) | 5-hydroxytryptamine receptor 1A (5HT1A) | 5HT1A_RAT | 5ht1a | G-21 | Htr1a | Serotonin 1 (5-HT1) receptor | Serotonin 1a (5-HT1a) receptor/Adrenergic receptor alpha-1 | Serotonin receptor 1A
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
46445.29
Organism:
Rattus norvegicus (rat)
Description:
Binding assays were performed using rat hippocampal membranes.
Residue:
422
Sequence:
MDVFSFGQGNNTTASQEPFGTGGNVTSISDVTFSYQVITSLLLGTLIFCAVLGNACVVAAIALERSLQNVANYLIGSLAVTDLMVSVLVLPMAALYQVLNKWTLGQVTCDLFIALDVLCCTSSILHLCAIALDRYWAITDPIDYVNKRTPRRAAALISLTWLIGFLISIPPMLGWRTPEDRSDPDACTISKDHGYTIYSTFGAFYIPLLLMLVLYGRIFRAARFRIRKTVRKVEKKGAGTSLGTSSAPPPKKSLNGQPGSGDWRRCAENRAVGTPCTNGAVRQGDDEATLEVIEVHRVGNSKEHLPLPSESGSNSYAPACLERKNERNAEAKRKMALARERKTVKTLGIIMGTFILCWLPFFIVALVLPFCESSCHMPALLGAIINWLGYSNSLLNPVIYAYFNKDFQNAFKKIIKCKFCRR
  
Inhibitor
Name:
BDBM29567
Synonyms:
1-(m-trifluorophenyl)piperazine, 14
Type:
Small organic molecule
Emp. Form.:
C23H28F3N3O2
Mol. Mass.:
435.4825
SMILES:
CC1=C(C)C(=O)N(C2CCC(CC2)N2CCN(CC2)c2cccc(c2)C(F)(F)F)C1=O |c:1,(-6.6,7.5,;-5.1,7.88,;-4.69,9.37,;-5.77,10.47,;-3.15,9.43,;-2.38,10.77,;-2.62,7.99,;-1.08,7.99,;-.31,9.32,;1.23,9.32,;2,7.99,;1.23,6.65,;-.31,6.65,;3.54,7.99,;4.28,9.34,;5.82,9.39,;6.62,8.08,;5.89,6.72,;4.35,6.68,;8.16,8.08,;8.91,6.73,;10.45,6.7,;11.24,8.02,;10.5,9.37,;8.96,9.39,;11.29,10.68,;9.97,11.47,;12.06,12.02,;12.62,9.9,;-3.82,7.03,;-3.82,5.49,)|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM21393
Synonyms:
7-(dipropylamino)-5,6,7,8-tetrahydronaphthalen-1-ol | 8-Hydroxy-2-(di-n-propylamino)tetralin | 8-OH-DPAT | 8-OH-DPAT,(+) | 8-OH-DPAT,(-) | 8-hydroxy-N,N-dipropylaminotetralin | CHEMBL1788118 | CHEMBL505765 | CHEMBL56 | DPAT | US10562853, Compound 8-OH-DPAT | [3H]-8-OH-DPAT | cid_1220
Type:
radiolabeled ligand
Emp. Form.:
C16H25NO
Mol. Mass.:
247.3758
SMILES:
CCCN(CCC)C1CCc2cccc(O)c2C1
Structure:
Search PDB for entries with ligand similarity: