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Assay Detail

CHEMBL782309

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

Functional
Compound tested in vitro for [Ca2+] influx into neonatal rat dorsal root ganglia (DRG)
30
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Vanilloid receptor (CHEMBL2096684)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Analogues of capsaicin with agonist activity as novel analgesic agents: structure-activity studies. 4. Potent, orally active analgesics.
Wrigglesworth R, Walpole CS, Bevan S, Campbell EA, Dray A, Hughes GA, James I, Masdin KJ, Winter J.
J Med Chem (1996) 39 : 4942 -4951
PubMed 8960554 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 30 6.15 7.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL146728 1 7.39
CHEMBL60744 1 7.25
CHEMBL144805 1 7.12
CHEMBL146099 1 6.89
CHEMBL424317 1 6.89
CHEMBL356291 1 6.77
CHEMBL76903 OLVANIL 2.0 1 6.77
CHEMBL147989 1 6.66
CHEMBL147909 1 6.60
CHEMBL294199 CAPSAICIN 4.0 1 6.52
CHEMBL344133 1 6.50
CHEMBL147791 1 6.48
CHEMBL356108 1 6.39
CHEMBL147716 1 6.32
CHEMBL357006 1 6.32
CHEMBL246648 1 6.29
CHEMBL144093 1 6.15
CHEMBL358974 2 6.02
CHEMBL356081 1 5.87
CHEMBL342313 1 5.78
CHEMBL148297 1 5.64
CHEMBL148121 1 5.57
CHEMBL359189 1 5.52
CHEMBL144517 1 5.45
CHEMBL342728 1 5.29
CHEMBL147045 1 5.21
CHEMBL358789 1 5.15
CHEMBL356959 1 4.28
CHEMBL146948 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL146728 EC50 = 41.0 nM 7.39
CHEMBL60744 EC50 = 56.0 nM 7.25
CHEMBL144805 EC50 = 75.0 nM 7.12
CHEMBL146099 EC50 = 130.0 nM 6.89
CHEMBL424317 EC50 = 130.0 nM 6.89
CHEMBL356291 EC50 = 170.0 nM 6.77
CHEMBL76903 OLVANIL EC50 = 170.0 nM 6.77
CHEMBL147989 EC50 = 220.0 nM 6.66
CHEMBL147909 EC50 = 250.0 nM 6.60
CHEMBL294199 CAPSAICIN EC50 = 300.0 nM 6.52
CHEMBL344133 EC50 = 320.0 nM 6.50
CHEMBL147791 EC50 = 330.0 nM 6.48
CHEMBL356108 EC50 = 410.0 nM 6.39
CHEMBL357006 EC50 = 480.0 nM 6.32
CHEMBL147716 EC50 = 480.0 nM 6.32
CHEMBL246648 EC50 = 510.0 nM 6.29
CHEMBL144093 EC50 = 710.0 nM 6.15
CHEMBL358974 EC50 = 950.0 nM 6.02
CHEMBL356081 EC50 = 1340.0 nM 5.87
CHEMBL342313 EC50 = 1660.0 nM 5.78
CHEMBL148297 EC50 = 2300.0 nM 5.64
CHEMBL148121 EC50 = 2720.0 nM 5.57
CHEMBL359189 EC50 = 3000.0 nM 5.52
CHEMBL144517 EC50 = 3520.0 nM 5.45
CHEMBL342728 EC50 = 5130.0 nM 5.29
CHEMBL358974 EC50 = 5480.0 nM 5.26
CHEMBL147045 EC50 = 6140.0 nM 5.21
CHEMBL358789 EC50 = 7030.0 nM 5.15
CHEMBL356959 EC50 = 53000.0 nM 4.28
CHEMBL146948 EC50 > 100000.0 nM -