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Assay Detail

CHEMBL4125475

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

Binding
Displacement of [3H]SP1-7 from NK1 receptor in Sprague-Dawley rat spinal cord membranes after 60 mins by scintillation counting method
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Spinal cord
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Substance-P receptor (CHEMBL4027)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

An imidazole based H-Phe-Phe-NH2 peptidomimetic with anti-allodynic effect in spared nerve injury mice.
Skogh A, Lesniak A, Sköld C, Karlgren M, Gaugaz FZ, Svensson R, Diwakarla S, Jonsson A, Fransson R, Nyberg F, Hallberg M, Sandström A.
Bioorg Med Chem Lett (2018) 28 : 2446 -2450
PubMed 29929882 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 8.70 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2397481 1 9.52
CHEMBL108438 1 8.82
CHEMBL589979 1 8.80
CHEMBL4127872 1 8.74
CHEMBL2396664 1 8.66
CHEMBL2042018 1 8.28
CHEMBL333357 ENDOMORPHIN 2 1 8.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2397481 Ki = 0.3 nM 9.52
CHEMBL108438 Ki = 1.5 nM 8.82
CHEMBL589979 Ki = 1.6 nM 8.80
CHEMBL4127872 Ki = 1.8 nM 8.74
CHEMBL2396664 Ki = 2.2 nM 8.66
CHEMBL2042018 Ki = 5.2 nM 8.28
CHEMBL333357 ENDOMORPHIN 2 Ki = 8.7 nM 8.06