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Assay Detail

CHEMBL884086

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

Functional
Inhibitory activity on acetylcholine-induced vasorelaxation of phenylephrine-precontracted rat aorta with intact endothelium
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Aorta
Confidence 1 — Organism
Curated By Expert

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

6-arylamino-5,8-quinolinediones and 7-arylamino-5,8-isoquinolinediones as inhibitors of endothelium-dependent vasorelaxation.
Ryu CK, Jung SH, Lee JA, Kim HJ, Lee SH, Chung JH.
Bioorg Med Chem Lett (1999) 9 : 2469 -2472
PubMed 10498190 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 28 6.39 6.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL55934 NAPHTHOQUINONE 1 6.90
CHEMBL81257 1 6.75
CHEMBL79405 1 6.72
CHEMBL315798 1 6.67
CHEMBL432368 1 6.66
CHEMBL84010 1 6.62
CHEMBL83341 1 6.60
CHEMBL84360 1 6.54
CHEMBL279994 1 6.54
CHEMBL79580 1 6.52
CHEMBL82885 1 6.48
CHEMBL312487 1 6.47
CHEMBL84014 1 6.44
CHEMBL81679 1 6.43
CHEMBL309680 1 6.37
CHEMBL83676 1 6.36
CHEMBL84282 1 6.35
CHEMBL310185 1 6.29
CHEMBL79264 1 6.27
CHEMBL311126 1 6.25
CHEMBL311720 1 6.22
CHEMBL83736 1 6.22
CHEMBL431395 1 6.19
CHEMBL315609 1 6.09
CHEMBL312124 1 6.03
CHEMBL227744 NITROARGININE 1.0 1 5.96
CHEMBL311957 1 5.95
CHEMBL316409 1 5.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL55934 NAPHTHOQUINONE EC50 = 127.0 nM 6.90
CHEMBL81257 EC50 = 178.0 nM 6.75
CHEMBL79405 EC50 = 190.0 nM 6.72
CHEMBL315798 EC50 = 214.0 nM 6.67
CHEMBL432368 EC50 = 220.0 nM 6.66
CHEMBL84010 EC50 = 239.0 nM 6.62
CHEMBL83341 EC50 = 251.0 nM 6.60
CHEMBL84360 EC50 = 290.0 nM 6.54
CHEMBL279994 EC50 = 288.0 nM 6.54
CHEMBL79580 EC50 = 302.0 nM 6.52
CHEMBL82885 EC50 = 330.0 nM 6.48
CHEMBL312487 EC50 = 335.0 nM 6.47
CHEMBL84014 EC50 = 362.0 nM 6.44
CHEMBL81679 EC50 = 374.0 nM 6.43
CHEMBL309680 EC50 = 430.0 nM 6.37
CHEMBL83676 EC50 = 439.0 nM 6.36
CHEMBL84282 EC50 = 449.0 nM 6.35
CHEMBL310185 EC50 = 519.0 nM 6.29
CHEMBL79264 EC50 = 541.0 nM 6.27
CHEMBL311126 EC50 = 562.0 nM 6.25
CHEMBL311720 EC50 = 607.0 nM 6.22
CHEMBL83736 EC50 = 603.0 nM 6.22
CHEMBL431395 EC50 = 640.0 nM 6.19
CHEMBL315609 EC50 = 805.0 nM 6.09
CHEMBL312124 EC50 = 937.0 nM 6.03
CHEMBL227744 NITROARGININE EC50 = 1100.0 nM 5.96
CHEMBL311957 EC50 = 1130.0 nM 5.95
CHEMBL316409 EC50 = 1230.0 nM 5.91