Target
Nuclear receptor subfamily 1 group I member 2
Ligand
BDBM50552412
Substrate
n/a
Meas. Tech.
ChEMBL_2034322 (CHEMBL4688480)
EC50
47000±n/a nM
Citation
 Kobayashi, JIHirasawa, HFujimori, YNakanishi, OKamada, NIkeda, TYamamoto, AKanbe, H Identification of N-acyl-N-indanyl-?-phenylglycinamides as selective TRPM8 antagonists designed to mitigate the risk of adverse effects. Bioorg Med Chem 30:0 (2021) [PubMed]  Article
Target
Name:
Nuclear receptor subfamily 1 group I member 2
Synonyms:
NR1I2 | NR1I2_HUMAN | Orphan nuclear receptor PAR1 | Orphan nuclear receptor PXR | PXR | Pregnane X receptor | SXR | Steroid and xenobiotic receptor | nuclear receptor subfamily 1 group I member 2 isoform 1
Type:
Nuclear receptor
Mol. Mass.:
49774.77
Organism:
Homo sapiens (Human)
Description:
O75469
Residue:
434
Sequence:
MEVRPKESWNHADFVHCEDTESVPGKPSVNADEEVGGPQICRVCGDKATGYHFNVMTCEGCKGFFRRAMKRNARLRCPFRKGACEITRKTRRQCQACRLRKCLESGMKKEMIMSDEAVEERRALIKRKKSERTGTQPLGVQGLTEEQRMMIRELMDAQMKTFDTTFSHFKNFRLPGVLSSGCELPESLQAPSREEAAKWSQVRKDLCSLKVSLQLRGEDGSVWNYKPPADSGGKEIFSLLPHMADMSTYMFKGIISFAKVISYFRDLPIEDQISLLKGAAFELCQLRFNTVFNAETGTWECGRLSYCLEDTAGGFQQLLLEPMLKFHYMLKKLQLHEEEYVLMQAISLFSPDRPGVLQHRVVDQLQEQFAITLKSYIECNRPQPAHRFLFLKIMAMLTELRSINAQHTQRLLRIQDIHPFATPLMQELFGITGS
  
Inhibitor
Name:
BDBM50552412
Synonyms:
CHEMBL4752955
Type:
Small organic molecule
Emp. Form.:
C23H19F2N3O2
Mol. Mass.:
407.4127
SMILES:
NC(=O)[C@H](N([C@@H]1CCc2c1cc(F)cc2F)C(=O)c1cccnc1)c1ccccc1 |r|
Structure:
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