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Assay Detail

CHEMBL1799418

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

Functional
Antitrypanosomal activity against Trypanosoma brucei brucei
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Trypanosoma brucei brucei
Confidence 1 — Organism
Curated By Autocuration

Target

Trypanosoma brucei brucei (CHEMBL612851)
Type ORGANISM
Organism Trypanosoma brucei brucei

Publication

SAR of 2-amino and 2,4-diamino pyrimidines with in vivo efficacy against Trypanosoma brucei.
Perales JB, Freeman J, Bacchi CJ, Bowling T, Don R, Gaukel E, Mercer L, Moore JA, Nare B, Nguyen TM, Noe RA, Randolph R, Rewerts C, Wring SA, Yarlett N, Jacobs RT.
Bioorg Med Chem Lett (2011) 21 : 2816 -2819
PubMed 21507639 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 6.32 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1795651 1 7.52
CHEMBL1795634 1 7.37
CHEMBL1795628 1 7.35
CHEMBL1795635 1 7.19
CHEMBL1795629 1 7.06
CHEMBL1795638 1 6.96
CHEMBL1795637 1 6.96
CHEMBL1795633 1 6.89
CHEMBL268507 1 6.77
CHEMBL1795652 1 6.77
CHEMBL1795639 1 6.72
CHEMBL1795653 1 6.58
CHEMBL1795631 1 6.54
CHEMBL1795640 1 6.54
CHEMBL1795656 1 6.51
CHEMBL1795654 1 6.48
CHEMBL1795626 1 6.47
CHEMBL1795641 1 6.44
CHEMBL1795627 1 6.43
CHEMBL1795636 1 6.39
CHEMBL1795349 1 6.24
CHEMBL216126 1 6.18
CHEMBL1795630 1 5.82
CHEMBL1795655 1 5.80
CHEMBL1795657 1 5.75
CHEMBL1795648 1 5.75
CHEMBL1795632 1 5.51
CHEMBL217537 1 5.48
CHEMBL1795644 1 5.35
CHEMBL1795643 1 5.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1795651 IC50 = 30.0 nM 7.52
CHEMBL1795634 IC50 = 43.0 nM 7.37
CHEMBL1795628 IC50 = 45.0 nM 7.35
CHEMBL1795635 IC50 = 65.0 nM 7.19
CHEMBL1795629 IC50 = 88.0 nM 7.06
CHEMBL1795638 IC50 = 110.0 nM 6.96
CHEMBL1795637 IC50 = 110.0 nM 6.96
CHEMBL1795633 IC50 = 130.0 nM 6.89
CHEMBL268507 IC50 = 170.0 nM 6.77
CHEMBL1795652 IC50 = 170.0 nM 6.77
CHEMBL1795639 IC50 = 190.0 nM 6.72
CHEMBL1795653 IC50 = 260.0 nM 6.58
CHEMBL1795631 IC50 = 290.0 nM 6.54
CHEMBL1795640 IC50 = 290.0 nM 6.54
CHEMBL1795656 IC50 = 310.0 nM 6.51
CHEMBL1795654 IC50 = 330.0 nM 6.48
CHEMBL1795626 IC50 = 340.0 nM 6.47
CHEMBL1795641 IC50 = 360.0 nM 6.44
CHEMBL1795627 IC50 = 370.0 nM 6.43
CHEMBL1795636 IC50 = 410.0 nM 6.39
CHEMBL1795349 IC50 = 570.0 nM 6.24
CHEMBL216126 IC50 = 660.0 nM 6.18
CHEMBL1795630 IC50 = 1530.0 nM 5.82
CHEMBL1795655 IC50 = 1600.0 nM 5.80
CHEMBL1795657 IC50 = 1800.0 nM 5.75
CHEMBL1795648 IC50 = 1800.0 nM 5.75
CHEMBL1795632 IC50 = 3100.0 nM 5.51
CHEMBL217537 IC50 = 3300.0 nM 5.48
CHEMBL1795644 IC50 = 4500.0 nM 5.35
CHEMBL1795643 IC50 = 4600.0 nM 5.34
CHEMBL1795646 IC50 = 5500.0 nM 5.26
CHEMBL1795647 IC50 = 7400.0 nM 5.13
CHEMBL1795649 IC50 = 10000.0 nM 5.00
CHEMBL1795650 IC50 > 12000.0 nM -
CHEMBL1795645 IC50 > 12000.0 nM -
CHEMBL1795642 IC50 > 11000.0 nM -
CHEMBL1795658 IC50 > 12000.0 nM -
CHEMBL387448 IC50 > 14000.0 nM -