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Assay Detail

CHEMBL1104447

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

Functional
Vasodilatory activity in Wistar rat endothelium-intact thoracic aortic strip assessed as inhibition of phenylephrine-induced contraction after 120 mins
14
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Aorta (CHEMBL613606)
Type TISSUE
Organism Rattus norvegicus

Publication

Synthesis and preliminary pharmacological characterisation of a new class of nitrogen-containing bisphosphonates (N-BPs).
Lolli ML, Rolando B, Tosco P, Chaurasia S, Di Stilo A, Lazzarato L, Gorassini E, Ferracini R, Oliaro-Bosso S, Fruttero R, Gasco A.
Bioorg Med Chem (2010) 18 : 2428 -2438
PubMed 20299227 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Inhibition 7 - -
EC50 7 5.26 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1093436 2 6.70
CHEMBL1091027 2 6.64
CHEMBL1088773 2 4.46
CHEMBL1090497 2 4.35
CHEMBL1093434 3 4.14
CHEMBL997 IBANDRONIC ACID 4.0 1 -
CHEMBL1091521 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1093436 EC50 = 200.0 nM 6.70
CHEMBL1091027 EC50 = 230.0 nM 6.64
CHEMBL1088773 EC50 = 35000.0 nM 4.46
CHEMBL1090497 EC50 = 45000.0 nM 4.35
CHEMBL1093434 EC50 = 73000.0 nM 4.14
CHEMBL997 IBANDRONIC ACID Inhibition - % -
CHEMBL1093434 Inhibition - % -
CHEMBL1093436 Inhibition - % -
CHEMBL1091521 Inhibition - % -
CHEMBL1091027 Inhibition - % -
CHEMBL1090497 Inhibition - % -
CHEMBL1088773 Inhibition - % -
CHEMBL1093434 EC50 - -
CHEMBL1091521 EC50 = 108000.0 nM -