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Target
Thyrotropin-releasing hormone receptor
Ligand
BDBM50196458
Substrate
n/a
Meas. Tech.
ChEMBL_431933 (CHEMBL917828)
EC50
17000±n/a nM
Citation
 Kaur, N; Monga, V; Lu, X; Gershengorn, MC; Jain, R Modifications of the pyroglutamic acid and histidine residues in thyrotropin-releasing hormone (TRH) yield analogs with selectivity for TRH receptor type 2 over type 1. Bioorg Med Chem 15:433-43 (2006) [PubMed]  Article 
Target
Name:
Thyrotropin-releasing hormone receptor
Synonyms:
TRFR_HUMAN | TRH-R | TRHR | Thyroliberin receptor
Type:
PROTEIN
Mol. Mass.:
45093.48
Organism:
Homo sapiens (Human)
Description:
ChEMBL_431933
Residue:
398
Sequence:
MENETVSELNQTQLQPRAVVALEYQVVTILLVLIICGLGIVGNIMVVLVVMRTKHMRTPTNCYLVSLAVADLMVLVAAGLPNITDSIYGSWVYGYVGCLCITYLQYLGINASSCSITAFTIERYIAICHPIKAQFLCTFSRAKKIIIFVWAFTSLYCMLWFFLLDLNISTYKDAIVISCGYKISRNYYSPIYLMDFGVFYVVPMILATVLYGFIARILFLNPIPSDPKENSKTWKNDSTHQNTNLNVNTSNRCFNSTVSSRKQVTKMLAVVVILFALLWMPYRTLVVVNSFLSSPFQENWFLLFCRICIYLNSAINPVIYNLMSQKFRAAFRKLCNCKQKPTEKPANYSVALNYSVIKESDHFSTELDDITVTDTYLSATKVSFDDTCLASEVSFSQS
  
Inhibitor
Name:
BDBM50196458
Synonyms:
(2S)-1-{(2S)-3-(1-benzyl-1H-4-imidazolyl)-2-[(2S)-6-oxohexahydro-2-pyridinylcarboxamido]azolane-propanoyl}azolane-2-carboxamide | CHEMBL389037
Type:
Small organic molecule
Emp. Form.:
C24H30N6O4
Mol. Mass.:
466.5328
SMILES:
NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cn(Cc2ccccc2)cn1)NC(=O)[C@@H]1CCCC(=O)N1
Structure:
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