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Assay Detail

CHEMBL5041223

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

Functional
Antinociceptive activity against Sprague-Dawley rat model of thermal stimuli induced nociception assessed as concentration required for maximal tail flick withdrawal latency administered subcutaneously as single dose measured up to 24 hrs by tail flick test
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

Development of ProTx-II Analogues as Highly Selective Peptide Blockers of Na<sub>v</sub>1.7 for the Treatment of Pain.
Adams GL, Pall PS, Grauer SM, Zhou X, Ballard JE, Vavrek M, Kraus RL, Morissette P, Li N, Colarusso S, Bianchi E, Palani A, Klein R, John CT, Wang D, Tudor M, Nolting AF, Biba M, Nowak T, Makarov AA, Reibarkh M, Buevich AV, Zhong W, Regalado EL, Wang X, Gao Q, Shahripour A, Zhu Y, de Simone D, Frattarelli T, Pasquini NM, Magotti P, Iaccarino R, Li Y, Solly K, Lee KJ, Wang W, Chen F, Zeng H, Wang J, Regan H, Amin RP, Regan CP, Burgey CS, Henze DA, Sun C, Tellers DM.
J Med Chem (2022) 65 : 485 -496
PubMed 34931831 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 6.16 6.53

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5085021 1 6.53
CHEMBL5076349 1 5.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5085021 EC50 = 294.0 nM 6.53
CHEMBL5076349 EC50 = 1619.0 nM 5.79