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Target
Nuclear receptor subfamily 1 group I member 2
Ligand
BDBM50026240
Substrate
n/a
Meas. Tech.
ChEMBL_1438948 (CHEMBL3382459)
EC50
>50000±n/a nM
Citation
 Wacker, DA; Wang, Y; Broekema, M; Rossi, K; O'Connor, S; Hong, Z; Wu, G; Malmstrom, SE; Hung, CP; LaMarre, L; Chimalakonda, A; Zhang, L; Xin, L; Cai, H; Chu, C; Boehm, S; Zalaznick, J; Ponticiello, R; Sereda, L; Han, SP; Zebo, R; Zinker, B; Luk, CE; Wong, R; Everlof, G; Li, YX; Wu, CK; Lee, M; Griffen, S; Miller, KJ; Krupinski, J; Robl, JA Discovery of 5-chloro-4-((1-(5-chloropyrimidin-2-yl)piperidin-4-yl)oxy)-1-(2-fluoro-4-(methylsulfonyl)phenyl)pyridin-2(1H)-one (BMS-903452), an antidiabetic clinical candidate targeting GPR119. J Med Chem 57:7499-508 (2014) [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:
BDBM50026240
Synonyms:
CHEMBL3338194
Type:
Small organic molecule
Emp. Form.:
C21H19Cl2FN4O4S
Mol. Mass.:
513.369
SMILES:
CS(=O)(=O)c1ccc(c(F)c1)-n1cc(Cl)c(OC2CCN(CC2)c2ncc(Cl)cn2)cc1=O
Structure:
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