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Assay Detail

CHEMBL776396

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Functional
In vitro calcium antagonist activity was assessed against calcium induced constriction of potassium-depolarized rat aorta
31
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Aorta
Confidence 1 — Organism
Curated By Autocuration

Publication

Long-acting dihydropyridine calcium antagonists. 1. 2-Alkoxymethyl derivatives incorporating basic substituents.
Arrowsmith JE, Campbell SF, Cross PE, Stubbs JK, Burges RA, Gardiner DG, Blackburn KJ.
J Med Chem (1986) 29 : 1696 -1702
PubMed 2943898 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 7.53 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1491 AMLODIPINE 4.0 3 8.70
CHEMBL300302 1 8.60
CHEMBL47909 1 8.50
CHEMBL297642 1 8.50
CHEMBL45450 1 8.40
CHEMBL49548 1 8.20
CHEMBL44640 1 8.10
CHEMBL49448 1 8.00
CHEMBL295913 1 8.00
CHEMBL296478 1 8.00
CHEMBL49742 1 7.90
CHEMBL294958 1 7.90
CHEMBL44804 1 7.90
CHEMBL49108 1 7.90
CHEMBL297828 1 7.90
CHEMBL46292 1 7.80
CHEMBL297871 1 7.80
CHEMBL45191 1 7.40
CHEMBL46190 1 7.40
CHEMBL297674 1 7.20
CHEMBL49709 1 7.20
CHEMBL45823 1 7.10
CHEMBL49743 1 6.90
CHEMBL47547 1 6.80
CHEMBL296229 1 6.80
CHEMBL295674 1 6.40
CHEMBL48141 1 6.10
CHEMBL44662 1 6.00
CHEMBL49949 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1491 AMLODIPINE IC50 = 1.995 nM 8.70
CHEMBL300302 IC50 = 2.512 nM 8.60
CHEMBL47909 IC50 = 3.162 nM 8.50
CHEMBL297642 IC50 = 3.162 nM 8.50
CHEMBL45450 IC50 = 3.981 nM 8.40
CHEMBL49548 IC50 = 6.31 nM 8.20
CHEMBL44640 IC50 = 7.943 nM 8.10
CHEMBL1491 AMLODIPINE IC50 = 7.943 nM 8.10
CHEMBL49448 IC50 = 10.0 nM 8.00
CHEMBL295913 IC50 = 10.0 nM 8.00
CHEMBL296478 IC50 = 10.0 nM 8.00
CHEMBL44804 IC50 = 12.59 nM 7.90
CHEMBL297828 IC50 = 12.59 nM 7.90
CHEMBL49108 IC50 = 12.59 nM 7.90
CHEMBL49742 IC50 = 12.59 nM 7.90
CHEMBL294958 IC50 = 12.59 nM 7.90
CHEMBL46292 IC50 = 15.85 nM 7.80
CHEMBL297871 IC50 = 15.85 nM 7.80
CHEMBL46190 IC50 = 39.81 nM 7.40
CHEMBL45191 IC50 = 39.81 nM 7.40
CHEMBL49709 IC50 = 63.1 nM 7.20
CHEMBL297674 IC50 = 63.1 nM 7.20
CHEMBL45823 IC50 = 79.43 nM 7.10
CHEMBL49743 IC50 = 125.89 nM 6.90
CHEMBL296229 IC50 = 158.49 nM 6.80
CHEMBL47547 IC50 = 158.49 nM 6.80
CHEMBL295674 IC50 = 398.11 nM 6.40
CHEMBL48141 IC50 = 794.33 nM 6.10
CHEMBL49949 IC50 = 1000.0 nM 6.00
CHEMBL44662 IC50 = 1000.0 nM 6.00
CHEMBL1491 AMLODIPINE IC50 = 1584.89 nM 5.80