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Assay Detail

CHEMBL3737673

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Functional
Vasodilative activity in isolated Sprague-Dawley rat Superior mesenteric arterial ring assessed as reduction in KCl-induced contraction by wire myograph method relative to control
ChEMBL ↗
50
Total Activities
25
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 3 — Cell-line / Tissue
Curated By Autocuration

Target

Molecular identity unknown (CHEMBL612546) ↗
Type UNKNOWN

Publication

Discovery of novel 2-benzylisoquinolin-1(2H)-ones as potent vasodilative agents.
Kang BR, Li S, Mao S, Cao YX, Zhang SQ.
Bioorg Med Chem Lett (2015) 25 : 5808 -5812
PubMed 26546216 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Rmax 25 - -
EC50 20 5.92 9.50
pEC50 5 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL475534 NITRENDIPINE 3.0 2 9.50
CHEMBL3735483 — — 2 6.70
CHEMBL3736391 — — 2 6.60
CHEMBL3734876 — — 2 6.40
CHEMBL3736500 — — 2 6.30
CHEMBL3735909 — — 2 6.30
CHEMBL3736068 — — 2 6.10
CHEMBL3736290 — — 2 6.00
CHEMBL3735294 — — 2 5.70
CHEMBL3736032 — — 2 5.70
CHEMBL3735351 — — 2 5.70
CHEMBL3734981 — — 2 5.60
CHEMBL3736344 — — 2 5.50
CHEMBL3735793 — — 2 5.50
CHEMBL3736370 — — 2 5.40
CHEMBL3735193 — — 2 5.40
CHEMBL3736352 — — 2 5.30
CHEMBL3736518 — — 2 5.20
CHEMBL3734775 — — 2 4.80
CHEMBL3734897 — — 2 4.60
CHEMBL3735177 — — 2 -
CHEMBL3736203 — — 2 -
CHEMBL3735089 — — 2 -
CHEMBL3735403 — — 2 -
CHEMBL3734807 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL475534 NITRENDIPINE EC50 = 0.3162 nM 9.50
CHEMBL3735483 — EC50 = 199.53 nM 6.70
CHEMBL3736391 — EC50 = 251.19 nM 6.60
CHEMBL3734876 — EC50 = 398.11 nM 6.40
CHEMBL3735909 — EC50 = 501.19 nM 6.30
CHEMBL3736500 — EC50 = 501.19 nM 6.30
CHEMBL3736068 — EC50 = 794.33 nM 6.10
CHEMBL3736290 — EC50 = 1000.0 nM 6.00
CHEMBL3736032 — EC50 = 1995.26 nM 5.70
CHEMBL3735351 — EC50 = 1995.26 nM 5.70
CHEMBL3735294 — EC50 = 1995.26 nM 5.70
CHEMBL3734981 — EC50 = 2511.89 nM 5.60
CHEMBL3736344 — EC50 = 3162.28 nM 5.50
CHEMBL3735793 — EC50 = 3162.28 nM 5.50
CHEMBL3736370 — EC50 = 3981.07 nM 5.40
CHEMBL3735193 — EC50 = 3981.07 nM 5.40
CHEMBL3736352 — EC50 = 5011.87 nM 5.30
CHEMBL3736518 — EC50 = 6309.57 nM 5.20
CHEMBL3734775 — EC50 = 15848.93 nM 4.80
CHEMBL3734897 — EC50 = 25118.86 nM 4.60
CHEMBL3736290 — Rmax = 76.4 % -
CHEMBL3736518 — Rmax = 89.5 % -
CHEMBL3734775 — Rmax = 73.1 % -
CHEMBL3735483 — Rmax = 106.5 % -
CHEMBL3735909 — Rmax = 75.3 % -
CHEMBL3734981 — Rmax = 71.3 % -
CHEMBL3735351 — Rmax = 67.4 % -
CHEMBL475534 NITRENDIPINE Rmax = 99.8 % -
CHEMBL3736370 — Rmax = 54.2 % -
CHEMBL3734876 — Rmax = 94.3 % -
CHEMBL3736068 — Rmax = 90.8 % -
CHEMBL3735294 — Rmax = 84.0 % -
CHEMBL3735193 — Rmax = 51.4 % -
CHEMBL3736352 — Rmax = 52.3 % -
CHEMBL3735793 — Rmax = 84.7 % -
CHEMBL3736500 — Rmax = 91.6 % -
CHEMBL3735403 — pEC50 - — -
CHEMBL3735089 — pEC50 - — -
CHEMBL3736203 — pEC50 - — -
CHEMBL3735177 — pEC50 - — -
CHEMBL3734807 — Rmax - — -
CHEMBL3735403 — Rmax - — -
CHEMBL3734807 — pEC50 - — -
CHEMBL3736203 — Rmax - — -
CHEMBL3735177 — Rmax - — -
CHEMBL3736344 — Rmax = 74.2 % -
CHEMBL3736032 — Rmax = 61.8 % -
CHEMBL3734897 — Rmax = 60.6 % -
CHEMBL3736391 — Rmax = 98.7 % -
CHEMBL3735089 — Rmax - — -