Target
Equilibrative nucleoside transporter 1
Ligand
BDBM23676
Substrate
BDBM23618
Meas. Tech.
Flow Cytometric Assay
Ki
14.7±n/a nM
IC50
260±n/a nM
Citation
 Lin, WBuolamwini, JK Synthesis, flow cytometric evaluation, and identification of highly potent dipyridamole analogues as equilibrative nucleoside transporter 1 inhibitors. J Med Chem 50:3906-20 (2007) [PubMed]  Article 
Target
Name:
Equilibrative nucleoside transporter 1
Synonyms:
ENT1 | Equilibrative NBMPR-sensitive nucleoside transporter | Equilibrative Nucleoside Transporter 1 (ENT1) | Equilibrative nitrobenzylmercaptopurine riboside-sensitive nucleoside transporter | Equilibrative nucleoside transporter 1 | Nucleoside transporter, es-type | S29A1_HUMAN | SLC29A1 | Solute carrier family 29 member 1
Type:
Multi-pass membrane protein
Mol. Mass.:
50225.92
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
456
Sequence:
MTTSHQPQDRYKAVWLIFFMLGLGTLLPWNFFMTATQYFTNRLDMSQNVSLVTAELSKDAQASAAPAAPLPERNSLSAIFNNVMTLCAMLPLLLFTYLNSFLHQRIPQSVRILGSLVAILLVFLITAILVKVQLDALPFFVITMIKIVLINSFGAILQGSLFGLAGLLPASYTAPIMSGQGLAGFFASVAMICAIASGSELSESAFGYFITACAVIILTIICYLGLPRLEFYRYYQQLKLEGPGEQETKLDLISKGEEPRAGKEESGVSVSNSQPTNESHSIKAILKNISVLAFSVCFIFTITIGMFPAVTVEVKSSIAGSSTWERYFIPVSCFLTFNIFDWLGRSLTAVFMWPGKDSRWLPSLVLARLVFVPLLLLCNIKPRRYLTVVFEHDAWFIFFMAAFAFSNGYLASLCMCFGPKKVKPAEAETAGAIMAFFLCLGLALGAVFSFLFRAIV
  
Inhibitor
Name:
BDBM23676
Synonyms:
2-({6-[bis(2-hydroxyethyl)amino]-4,8-bis[(2,2-dimethylpropyl)amino]pyrimido[5,4-d][1,3]diazin-2-yl}(2-hydroxyethyl)amino)ethan-1-ol | Dipyridamole Analogue, 58
Type:
Small organic molecule
Emp. Form.:
C24H44N8O4
Mol. Mass.:
508.6574
SMILES:
CC(C)(C)CNc1nc(nc2c(NCC(C)(C)C)nc(nc12)N(CCO)CCO)N(CCO)CCO
Structure:
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Substrate
Name:
BDBM23618
Synonyms:
5-(SAENTA)-X8-fluorescein | 5-[(5-{[2-({[(2S,3S,4R,5R)-3,4-dihydroxy-5-(6-{[(4-nitrophenyl)methyl]amino}-9H-purin-9-yl)oxolan-2-yl]methyl}sulfanyl)ethyl]carbamoyl}pentyl)carbamoyl]-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid
Type:
Fluorescent probe
Emp. Form.:
C46H44N8O12S
Mol. Mass.:
932.953
SMILES:
O[C@@H]1[C@@H](CSCCNC(=O)CCCCCNC(=O)c2ccc(c(c2)C(O)=O)-c2c3ccc(O)cc3oc3cc(=O)ccc23)O[C@H]([C@@H]1O)n1cnc2c(NCc3ccc(cc3)[N+]([O-])=O)ncnc12 |r,wU:2.2,44.51,wD:1.0,45.50,(15.72,-6.42,;16.68,-5.22,;16.26,-3.73,;16.26,-2.19,;14.93,-1.42,;13.6,-2.19,;12.26,-1.42,;10.93,-2.19,;9.6,-1.42,;9.6,.12,;8.26,-2.19,;6.93,-1.42,;5.59,-2.19,;4.26,-1.42,;2.93,-2.19,;1.59,-1.42,;.26,-2.19,;.26,-3.73,;-1.07,-1.42,;-2.41,-2.19,;-3.74,-1.42,;-3.74,.12,;-2.41,.89,;-1.07,.12,;-2.41,2.43,;-.88,2.63,;-2.81,3.91,;-5.07,.89,;-6.41,.12,;-6.41,-1.42,;-7.74,-2.19,;-9.08,-1.42,;-10.41,-2.19,;-9.08,.12,;-7.74,.89,;-7.74,2.43,;-6.41,3.2,;-6.41,4.74,;-5.07,5.51,;-5.07,7.05,;-3.74,4.74,;-3.74,3.2,;-5.07,2.43,;17.55,-2.88,;18.75,-3.84,;18.22,-5.28,;19.07,-6.56,;19.15,-2.35,;18.22,-1.12,;19.1,.14,;20.58,-.31,;21.9,.49,;21.87,2.03,;23.2,2.8,;24.54,2.03,;25.87,2.8,;27.2,2.03,;27.2,.49,;25.87,-.28,;24.54,.49,;28.54,-.28,;28.54,-1.82,;29.87,.49,;23.25,-.26,;23.27,-1.8,;21.96,-2.59,;20.61,-1.85,)|
Structure:
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