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Assay Detail

CHEMBL3611368

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

Functional
Increase in coronary flow in Wistar rat Langendorff isolated perfused heart
20
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Heart
Confidence 1 — Organism
Curated By Autocuration

Target

Heart (CHEMBL613629)
Type TISSUE
Organism Rattus norvegicus

Publication

Discovery of novel bridged tetrahydronaphthalene derivatives as potent T/L-type calcium channel blockers.
Renneberg D, Hubler F, Rey M, Hess P, Delahaye S, Gatfield J, Iglarz M, Hilpert K.
Bioorg Med Chem Lett (2015) 25 : 3941 -3946
PubMed 26231163 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 7.48 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3609819 1 8.15
CHEMBL3608316 1 7.80
CHEMBL3609822 1 7.70
CHEMBL3608941 1 7.70
CHEMBL3609818 1 7.66
CHEMBL3609824 1 7.64
CHEMBL45816 MIBEFRADIL 4.0 1 7.58
CHEMBL3608947 2 7.58
CHEMBL3609817 1 7.58
CHEMBL3609825 1 7.54
CHEMBL3608943 1 7.42
CHEMBL3608940 1 7.40
CHEMBL3608945 2 7.38
CHEMBL3608946 1 7.11
CHEMBL3608942 1 6.87
CHEMBL3608944 1 6.60
CHEMBL3609821 1 -
CHEMBL3609820 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3609819 EC50 = 7.0 nM 8.15
CHEMBL3608316 EC50 = 16.0 nM 7.80
CHEMBL3609822 EC50 = 20.0 nM 7.70
CHEMBL3608941 EC50 = 20.0 nM 7.70
CHEMBL3609818 EC50 = 22.0 nM 7.66
CHEMBL3609824 EC50 = 23.0 nM 7.64
CHEMBL45816 MIBEFRADIL EC50 = 26.0 nM 7.58
CHEMBL3608947 EC50 = 26.0 nM 7.58
CHEMBL3609817 EC50 = 26.0 nM 7.58
CHEMBL3609825 EC50 = 29.0 nM 7.54
CHEMBL3608943 EC50 = 38.0 nM 7.42
CHEMBL3608947 EC50 = 39.0 nM 7.41
CHEMBL3608940 EC50 = 40.0 nM 7.40
CHEMBL3608945 EC50 = 42.0 nM 7.38
CHEMBL3608946 EC50 = 77.0 nM 7.11
CHEMBL3608942 EC50 = 134.0 nM 6.87
CHEMBL3608944 EC50 = 250.0 nM 6.60
CHEMBL3609821 EC50 > 1000.0 nM -
CHEMBL3608945 EC50 > 150.0 nM -
CHEMBL3609820 EC50 > 300.0 nM -