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Target
Mu-type opioid receptor
Ligand
BDBM278400
Substrate
n/a
Meas. Tech.
ChEMBL_1859528 (CHEMBL4360384)
IC50
60000±n/a nM
Citation
 Finlay, MRV; Anderton, M; Bailey, A; Boyd, S; Brookfield, J; Cairnduff, C; Charles, M; Cheasty, A; Critchlow, SE; Culshaw, J; Ekwuru, T; Hollingsworth, I; Jones, N; Leroux, F; Littleson, M; McCarron, H; McKelvie, J; Mooney, L; Nissink, JWM; Perkins, D; Powell, S; Quesada, MJ; Raubo, P; Sabin, V; Smith, J; Smith, PD; Stark, A; Ting, A; Wang, P; Wilson, Z; Winter-Holt, JJ; Wood, JM; Wrigley, GL; Yu, G; Zhang, P Discovery of a Thiadiazole-Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models. J Med Chem 62:6540-6560 (2019) [PubMed]  Article
Target
Name:
Mu-type opioid receptor
Synonyms:
M-OR-1 | MOP | MOR-1 | MOR1 | MUOR1 | Mu Opioid Receptor | Mu opiate receptor | OPIATE Mu | OPRM1 | OPRM_HUMAN | hMOP | mu-type opioid receptor isoform MOR-1
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
44789.51
Organism:
Homo sapiens (Human)
Description:
P35372
Residue:
400
Sequence:
MDSSAAPTNASNCTDALAYSSCSPAPSPGSWVNLSHLDGNLSDPCGPNRTDLGGRDSLCPPTGSPSMITAITIMALYSIVCVVGLFGNFLVMYVIVRYTKMKTATNIYIFNLALADALATSTLPFQSVNYLMGTWPFGTILCKIVISIDYYNMFTSIFTLCTMSVDRYIAVCHPVKALDFRTPRNAKIINVCNWILSSAIGLPVMFMATTKYRQGSIDCTLTFSHPTWYWENLLKICVFIFAFIMPVLIITVCYGLMILRLKSVRMLSGSKEKDRNLRRITRMVLVVVAVFIVCWTPIHIYVIIKALVTIPETTFQTVSWHFCIALGYTNSCLNPVLYAFLDENFKRCFREFCIPTSSNIEQQNSTRIRQNTRDHPSTANTVDRTNHQLENLEAETAPLP
  
Inhibitor
Name:
BDBM278400
Synonyms:
(2S)-2-Methoxy-2-phenyl-N-[5-[[(3R)-1-pyridazin-3-ylpyrrolidin-3-yl]amino]-1,3,4-thiadiazol-2-yl]acetamide | BDBM278426 | US10040788, Example 2(a) | US10294221, Example 20(b)
Type:
Small organic molecule
Emp. Form.:
C19H21N7O2S
Mol. Mass.:
411.481
SMILES:
CO[C@H](C(=O)Nc1nnc(N[C@@H]2CCN(C2)c2cccnn2)s1)c1ccccc1 |r|
Structure:
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