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Assay Detail

CHEMBL3761384

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Binding
Inhibition of voltage-gated calcium channel in Wistar rat synaptoneurosomes after 30 mins by fluorescent ratiometric indicator method
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Polycyclic amines as chloroquine resistance modulating agents in Plasmodium falciparum.
Joubert J, Kapp E, Taylor D, Smith PJ, Malan SF.
Bioorg Med Chem Lett (2016) 26 : 1151 -1155
PubMed 26832222 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.56 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1428 NIMODIPINE 4.0 1 8.10
CHEMBL1830325 1 6.57
CHEMBL6966 VERAPAMIL 4.0 1 6.48
CHEMBL3758459 1 6.32
CHEMBL3759841 1 6.01
CHEMBL1189234 1 4.46
CHEMBL391409 1 4.07
CHEMBL3758822 1 4.00
CHEMBL1830320 1 4.00
CHEMBL50588 EMETINE 4.0 1 -
CHEMBL76 CHLOROQUINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1428 NIMODIPINE IC50 = 8.0 nM 8.10
CHEMBL1830325 IC50 = 270.0 nM 6.57
CHEMBL6966 VERAPAMIL IC50 = 330.0 nM 6.48
CHEMBL3758459 IC50 = 480.0 nM 6.32
CHEMBL3759841 IC50 = 980.0 nM 6.01
CHEMBL1189234 IC50 = 35000.0 nM 4.46
CHEMBL391409 IC50 = 86000.0 nM 4.07
CHEMBL3758822 IC50 = 100000.0 nM 4.00
CHEMBL1830320 IC50 = 100000.0 nM 4.00
CHEMBL50588 EMETINE IC50 - -
CHEMBL76 CHLOROQUINE IC50 - -