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Target
Proton-coupled folate transporter
Ligand
BDBM66082
Substrate
n/a
Meas. Tech.
ChEMBL_1759624 (CHEMBL4194632)
IC50
121±n/a nM
Citation
 Ravindra, M; Wallace-Povirk, A; Karim, MA; Wilson, MR; O'Connor, C; White, K; Kushner, J; Polin, L; George, C; Hou, Z; Matherly, LH; Gangjee, A Tumor Targeting with Novel Pyridyl 6-Substituted Pyrrolo[2,3- d]Pyrimidine Antifolates via Cellular Uptake by Folate Receptor ? and the Proton-Coupled Folate Transporter and Inhibition of De Novo Purine Nucleotide Biosynthesis. J Med Chem 61:2027-2040 (2018) [PubMed]  Article 
Target
Name:
Proton-coupled folate transporter
Synonyms:
G21 | HCP1 | Heme carrier protein 1 | PCFT | PCFT/HCP1 | PCFT_HUMAN | SLC46A1 | Solute carrier family 46 member 1
Type:
PROTEIN
Mol. Mass.:
49782.13
Organism:
Homo sapiens (Human)
Description:
ChEMBL_1469597
Residue:
459
Sequence:
MEGSASPPEKPRARPAAAVLCRGPVEPLVFLANFALVLQGPLTTQYLWHRFSADLGYNGTRQRGGCSNRSADPTMQEVETLTSHWTLYMNVGGFLVGLFSSTLLGAWSDSVGRRPLLVLASLGLLLQALVSVFVVQLQLHVGYFVLGRILCALLGDFGGLLAASFASVADVSSSRSRTFRMALLEASIGVAGMLASLLGGHWLRAQGYANPFWLALALLIAMTLYAAFCFGETLKEPKSTRLFTFRHHRSIVQLYVAPAPEKSRKHLALYSLAIFVVITVHFGAQDILTLYELSTPLCWDSKLIGYGSAAQHLPYLTSLLALKLLQYCLADAWVAEIGLAFNILGMVVFAFATITPLMFTGYGLLFLSLVITPVIRAKLSKLVRETEQGALFSAVACVNSLAMLTASGIFNSLYPATLNFMKGFPFLLGAGLLLIPAVLIGMLEKADPHLEFQQFPQSP
  
Inhibitor
Name:
BDBM66082
Synonyms:
(2S)-2-[[4-[(2,4-diaminopteridin-6-yl)methyl-methyl-amino]benzoyl]amino]glutaric acid;hydrate | (2S)-2-[[4-[(2,4-diaminopteridin-6-yl)methyl-methylamino]benzoyl]amino]pentanedioic acid;hydrate | (2S)-2-[[4-[[2,4-bis(azanyl)pteridin-6-yl]methyl-methyl-amino]phenyl]carbonylamino]pentanedioic acid;hydrate | (2S)-2-[[[4-[(2,4-diamino-6-pteridinyl)methyl-methylamino]phenyl]-oxomethyl]amino]pentanedioic acid;hydrate | L-Glutamic acid, N-[4-[[(2,4-diamino-6-pteridinyl)methyl]methylamino]benzoyl]- [CAS] | MLS001401431 | SMR000449324 | US11530198, Example Methotrexate | cid_165528
Type:
Small organic molecule
Emp. Form.:
C20H22N8O5
Mol. Mass.:
454.4393
SMILES:
CN(Cc1cnc2nc(N)nc(N)c2n1)c1ccc(cc1)C(=O)N[C@@H](CCC(O)=O)C(O)=O
Structure:
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