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Assay Detail

CHEMBL3865046

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

Binding
Inhibition of recombinant Plasmodium falciparum CDPK4 expressed in Escherichia coli Rosetta Oxford using Syntide 2 as substrate assessed as decrease in depletion of ATP by Kinase glo luciferase assay
28
Total Activities
28
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

5-Aminopyrazole-4-carboxamide analogues are selective inhibitors of Plasmodium falciparum microgametocyte exflagellation and potential malaria transmission blocking agents.
Huang W, Hulverson MA, Zhang Z, Choi R, Hart KJ, Kennedy M, Vidadala RSR, Maly DJ, Van Voorhis WC, Lindner SE, Fan E, Ojo KK.
Bioorg Med Chem Lett (2016) 26 : 5487 -5491
PubMed 27780638 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 7.16 7.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3108997 1 7.51
CHEMBL3108998 1 7.44
CHEMBL3109011 1 7.43
CHEMBL3108912 1 7.41
CHEMBL3770409 1 7.36
CHEMBL3770142 1 7.32
CHEMBL3770980 1 7.31
CHEMBL3770425 1 7.24
CHEMBL3771306 1 7.24
CHEMBL3985876 1 7.15
CHEMBL3108913 1 7.13
CHEMBL3908956 1 7.13
CHEMBL3770299 1 7.12
CHEMBL3108991 1 7.11
CHEMBL3770649 1 7.10
CHEMBL3770743 1 7.09
CHEMBL3922900 1 7.09
CHEMBL3770313 1 7.09
CHEMBL3769900 1 7.09
CHEMBL3769798 1 7.08
CHEMBL3769623 1 7.05
CHEMBL3770760 1 7.03
CHEMBL3770802 1 7.03
CHEMBL3108986 1 7.03
CHEMBL3922004 1 6.99
CHEMBL3973192 1 6.99
CHEMBL3956316 1 6.95
CHEMBL3916476 1 6.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3108997 IC50 = 31.0 nM 7.51
CHEMBL3108998 IC50 = 36.0 nM 7.44
CHEMBL3109011 IC50 = 37.0 nM 7.43
CHEMBL3108912 IC50 = 39.0 nM 7.41
CHEMBL3770409 IC50 = 44.0 nM 7.36
CHEMBL3770142 IC50 = 48.0 nM 7.32
CHEMBL3770980 IC50 = 49.0 nM 7.31
CHEMBL3770425 IC50 = 57.0 nM 7.24
CHEMBL3771306 IC50 = 58.0 nM 7.24
CHEMBL3985876 IC50 = 71.0 nM 7.15
CHEMBL3108913 IC50 = 74.0 nM 7.13
CHEMBL3908956 IC50 = 74.0 nM 7.13
CHEMBL3770299 IC50 = 75.0 nM 7.12
CHEMBL3108991 IC50 = 77.0 nM 7.11
CHEMBL3770649 IC50 = 79.0 nM 7.10
CHEMBL3770743 IC50 = 81.0 nM 7.09
CHEMBL3922900 IC50 = 82.0 nM 7.09
CHEMBL3770313 IC50 = 82.0 nM 7.09
CHEMBL3769900 IC50 = 82.0 nM 7.09
CHEMBL3769798 IC50 = 83.0 nM 7.08
CHEMBL3769623 IC50 = 90.0 nM 7.05
CHEMBL3770760 IC50 = 94.0 nM 7.03
CHEMBL3770802 IC50 = 94.0 nM 7.03
CHEMBL3108986 IC50 = 94.0 nM 7.03
CHEMBL3922004 IC50 = 102.0 nM 6.99
CHEMBL3973192 IC50 = 103.0 nM 6.99
CHEMBL3956316 IC50 = 113.0 nM 6.95
CHEMBL3916476 IC50 = 123.0 nM 6.91