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Target
Synaptic vesicular amine transporter
Ligand
BDBM291687
Substrate
n/a
Meas. Tech.
ChEMBL_2249116 (CHEMBL5163326)
IC50
1800±n/a nM
Citation
 Huang, Y; Sendzik, M; Zhang, J; Gao, Z; Sun, Y; Wang, L; Gu, J; Zhao, K; Yu, Z; Zhang, L; Zhang, Q; Blanz, J; Chen, Z; Dubost, V; Fang, D; Feng, L; Fu, X; Kiffe, M; Li, L; Luo, F; Luo, X; Mi, Y; Mistry, P; Pearson, D; Piaia, A; Scheufler, C; Terranova, R; Weiss, A; Zeng, J; Zhang, H; Zhang, J; Zhao, M; Dillon, MP; Jeay, S; Qi, W; Moggs, J; Pissot-Soldermann, C; Li, E; Atadja, P; Lingel, A; Oyang, C Discovery of the Clinical Candidate MAK683: An EED-Directed, Allosteric, and Selective PRC2 Inhibitor for the Treatment of Advanced Malignancies. J Med Chem 65:5317-5333 (2022) [PubMed] 
Target
Name:
Synaptic vesicular amine transporter
Synonyms:
Monoamine transporter | SLC18A2 | SVMT | Solute carrier family 18 member 2 | VAT2 | VMAT2 | VMAT2_HUMAN | Vesicular amine transporter 2
Type:
PROTEIN
Mol. Mass.:
55709.61
Organism:
Homo sapiens (Human)
Description:
ChEMBL_610810
Residue:
514
Sequence:
MALSELALVRWLQESRRSRKLILFIVFLALLLDNMLLTVVVPIIPSYLYSIKHEKNATEIQTARPVHTASISDSFQSIFSYYDNSTMVTGNATRDLTLHQTATQHMVTNASAVPSDCPSEDKDLLNENVQVGLLFASKATVQLITNPFIGLLTNRIGYPIPIFAGFCIMFVSTIMFAFSSSYAFLLIARSLQGIGSSCSSVAGMGMLASVYTDDEERGNVMGIALGGLAMGVLVGPPFGSVLYEFVGKTAPFLVLAALVLLDGAIQLFVLQPSRVQPESQKGTPLTTLLKDPYILIAAGSICFANMGIAMLEPALPIWMMETMCSRKWQLGVAFLPASISYLIGTNIFGILAHKMGRWLCALLGMIIVGVSILCIPFAKNIYGLIAPNFGVGFAIGMVDSSMMPIMGYLVDLRHVSVYGSVYAIADVAFCMGYAIGPSAGGAIAKAIGFPWLMTIIGIIDILFAPLCFFLRSPPAKEEKMAILMDHNCPIKTKMYTQNNIQSYPIGEDEESESD
  
Inhibitor
Name:
BDBM291687
Synonyms:
N-((5-Fluoro-2,3-dihydrobenzofuran-4-yl)methyl)-8-(2-methylpyridin-3-yl)-[1,2,4]triazolo[4,3-c]pyrimidin-5-amine | US11207325, Example 2 | US9580437, Example 2
Type:
Small organic molecule
Emp. Form.:
C20H17FN6O
Mol. Mass.:
376.387
SMILES:
Cc1ncccc1-c1cnc(NCc2c3CCOc3ccc2F)n2cnnc12
Structure:
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