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Assay Detail

CHEMBL2157771

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of Plasmodium falciparum recombinant HGPRT expressed in Escherichia coli using Prib-PP as substrate by spectrophotometric assay in presence of guanine
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Plasmodium falciparum
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis of novel N-branched acyclic nucleoside phosphonates as potent and selective inhibitors of human, Plasmodium falciparum and Plasmodium vivax 6-oxopurine phosphoribosyltransferases.
Hocková D, Keough DT, Janeba Z, Wang TH, de Jersey J, Guddat LW.
J Med Chem (2012) 55 : 6209 -6223
PubMed 22725979 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 6.20 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2153484 1 7.00
CHEMBL2153477 1 7.00
CHEMBL2153487 1 7.00
CHEMBL2153490 1 6.70
CHEMBL2153483 1 6.70
CHEMBL2153497 1 6.70
CHEMBL2153480 1 6.70
CHEMBL2153485 1 6.52
CHEMBL2153493 1 6.40
CHEMBL2153496 1 6.40
CHEMBL2153492 1 6.22
CHEMBL2153482 1 6.16
CHEMBL2153478 1 5.89
CHEMBL2153476 1 5.77
CHEMBL2153486 1 5.72
CHEMBL2153495 1 5.58
CHEMBL2153481 1 5.40
CHEMBL2153491 1 5.22
CHEMBL2153498 1 4.80
CHEMBL2153489 1 -
CHEMBL2153479 1 -
CHEMBL2153488 1 -
CHEMBL2153494 1 -
CHEMBL2153499 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2153484 Ki = 100.0 nM 7.00
CHEMBL2153477 Ki = 100.0 nM 7.00
CHEMBL2153487 Ki = 100.0 nM 7.00
CHEMBL2153490 Ki = 200.0 nM 6.70
CHEMBL2153483 Ki = 200.0 nM 6.70
CHEMBL2153497 Ki = 200.0 nM 6.70
CHEMBL2153480 Ki = 200.0 nM 6.70
CHEMBL2153485 Ki = 300.0 nM 6.52
CHEMBL2153493 Ki = 400.0 nM 6.40
CHEMBL2153496 Ki = 400.0 nM 6.40
CHEMBL2153492 Ki = 600.0 nM 6.22
CHEMBL2153482 Ki = 700.0 nM 6.16
CHEMBL2153478 Ki = 1300.0 nM 5.89
CHEMBL2153476 Ki = 1700.0 nM 5.77
CHEMBL2153486 Ki = 1900.0 nM 5.72
CHEMBL2153495 Ki = 2600.0 nM 5.58
CHEMBL2153481 Ki = 4000.0 nM 5.40
CHEMBL2153491 Ki = 6000.0 nM 5.22
CHEMBL2153498 Ki = 16000.0 nM 4.80
CHEMBL2153489 Ki >= 250000.0 nM -
CHEMBL2153479 Ki - -
CHEMBL2153488 Ki >= 220000.0 nM -
CHEMBL2153494 Ki >= 210000.0 nM -
CHEMBL2153499 Ki >= 200000.0 nM -