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Assay Detail

CHEMBL3375499

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

Binding
Displacement of [3H]-SP1-7 from NK1 receptor (unknown origin) by scintillation counting analysis
9
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Substance-P receptor (CHEMBL249)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Exploration and pharmacokinetic profiling of phenylalanine based carbamates as novel substance p 1-7 analogues.
Fransson R, Nordvall G, Bylund J, Carlsson-Jonsson A, Kratz JM, Svensson R, Artursson P, Hallberg M, Sandström A.
ACS Med Chem Lett (2014) 5 : 1272 -1277
PubMed 25516784 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.97 8.38
Ki 3 8.59 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL108438 1 8.82
CHEMBL2396664 1 8.66
CHEMBL3358422 1 8.38
CHEMBL2042018 2 8.28
CHEMBL3358423 1 8.19
CHEMBL3358424 1 8.05
CHEMBL3358420 1 7.78
CHEMBL3358421 1 7.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL108438 Ki = 1.5 nM 8.82
CHEMBL2396664 Ki = 2.2 nM 8.66
CHEMBL3358422 IC50 = 4.2 nM 8.38
CHEMBL2042018 Ki = 5.2 nM 8.28
CHEMBL2042018 IC50 = 6.2 nM 8.21
CHEMBL3358423 IC50 = 6.5 nM 8.19
CHEMBL3358424 IC50 = 9.0 nM 8.05
CHEMBL3358420 IC50 = 16.5 nM 7.78
CHEMBL3358421 IC50 = 60.6 nM 7.22