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Assay Detail

CHEMBL894050

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Binding
Inhibition of ENT1 in human K562 cells by flow cytometric assay
ChEMBL ↗
164
Total Activities
82
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type K562
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Equilibrative nucleoside transporter 1 (CHEMBL1997) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, flow cytometric evaluation, and identification of highly potent dipyridamole analogues as equilibrative nucleoside transporter 1 inhibitors.
Lin W, Buolamwini JK.
J Med Chem (2007) 50 : 3906 -3920
PubMed 17636949 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 82 6.08 8.12
Ki 82 7.33 9.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL418509 NITROBENZYLMERCAPTOPURINE RIBONUCLEOSIDE — 2 9.37
CHEMBL243304 — — 2 9.31
CHEMBL242657 — — 2 9.11
CHEMBL243096 — — 2 9.07
CHEMBL242027 — — 2 8.37
CHEMBL932 DIPYRIDAMOLE 4.0 2 8.09
CHEMBL442098 — — 2 8.09
CHEMBL389137 — — 2 7.83
CHEMBL396717 — — 2 7.80
CHEMBL395529 — — 2 7.78
CHEMBL388875 — — 2 7.77
CHEMBL437946 — — 2 7.67
CHEMBL429101 — — 2 7.42
CHEMBL243119 — — 2 7.42
CHEMBL395264 — — 2 7.28
CHEMBL183236 — — 2 7.04
CHEMBL242868 — — 2 7.00
CHEMBL242445 — — 2 6.98
CHEMBL243548 — — 2 6.92
CHEMBL242893 — — 2 6.87
CHEMBL395530 — — 2 6.85
CHEMBL242890 — — 2 6.72
CHEMBL243524 — — 2 6.71
CHEMBL242009 — — 2 6.67
CHEMBL396716 — — 2 6.66
CHEMBL92870 LIDOFLAZINE 2.0 2 6.55
CHEMBL397453 — — 2 6.52
CHEMBL182365 — — 2 6.49
CHEMBL388703 — — 2 6.41
CHEMBL242647 — — 2 6.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL418509 NITROBENZYLMERCAPTOPURINE RIBONUCLEOSIDE Ki = 0.43 nM 9.37
CHEMBL243304 — Ki = 0.49 nM 9.31
CHEMBL242657 — Ki = 0.77 nM 9.11
CHEMBL243096 — Ki = 0.86 nM 9.07
CHEMBL242027 — Ki = 4.3 nM 8.37
CHEMBL418509 NITROBENZYLMERCAPTOPURINE RIBONUCLEOSIDE IC50 = 7.6 nM 8.12
CHEMBL932 DIPYRIDAMOLE Ki = 8.18 nM 8.09
CHEMBL442098 — Ki = 8.2 nM 8.09
CHEMBL243304 — IC50 = 8.67 nM 8.06
CHEMBL242657 — IC50 = 13.6 nM 7.87
CHEMBL389137 — Ki = 14.7 nM 7.83
CHEMBL243096 — IC50 = 15.2 nM 7.82
CHEMBL396717 — Ki = 15.8 nM 7.80
CHEMBL395529 — Ki = 16.8 nM 7.78
CHEMBL388875 — Ki = 17.1 nM 7.77
CHEMBL437946 — Ki = 21.2 nM 7.67
CHEMBL429101 — Ki = 38.0 nM 7.42
CHEMBL243119 — Ki = 38.0 nM 7.42
CHEMBL395264 — Ki = 53.1 nM 7.28
CHEMBL242027 — IC50 = 76.0 nM 7.12
CHEMBL183236 — Ki = 91.6 nM 7.04
CHEMBL242868 — Ki = 99.7 nM 7.00
CHEMBL242445 — Ki = 104.1 nM 6.98
CHEMBL243548 — Ki = 120.7 nM 6.92
CHEMBL242893 — Ki = 136.0 nM 6.87
CHEMBL395530 — Ki = 139.9 nM 6.85
CHEMBL442098 — IC50 = 145.0 nM 6.84
CHEMBL932 DIPYRIDAMOLE IC50 = 144.8 nM 6.84
CHEMBL242890 — Ki = 191.0 nM 6.72
CHEMBL243524 — Ki = 193.0 nM 6.71
CHEMBL242009 — Ki = 216.4 nM 6.67
CHEMBL396716 — Ki = 216.7 nM 6.66
CHEMBL389137 — IC50 = 260.0 nM 6.58
CHEMBL92870 LIDOFLAZINE Ki = 279.9 nM 6.55
CHEMBL396717 — IC50 = 279.7 nM 6.55
CHEMBL395529 — IC50 = 297.0 nM 6.53
CHEMBL388875 — IC50 = 302.0 nM 6.52
CHEMBL397453 — Ki = 300.0 nM 6.52
CHEMBL182365 — Ki = 325.2 nM 6.49
CHEMBL437946 — IC50 = 375.0 nM 6.43
CHEMBL388703 — Ki = 393.0 nM 6.41
CHEMBL242647 — Ki = 427.6 nM 6.37
CHEMBL398221 — Ki = 449.0 nM 6.35
CHEMBL395528 — Ki = 489.0 nM 6.31
CHEMBL429101 — IC50 = 672.0 nM 6.17
CHEMBL243119 — IC50 = 673.0 nM 6.17
CHEMBL242656 — Ki = 690.9 nM 6.16
CHEMBL395264 — IC50 = 940.0 nM 6.03
CHEMBL183236 — IC50 = 1621.0 nM 5.79
CHEMBL242868 — IC50 = 1764.0 nM 5.75