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Assay Detail

CHEMBL3738442

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

Binding
Displacement of [3H]SP from rat neurokinin-1 receptor expressed in CHO cells incubated for 20 mins by liquid scintillation counting
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of Novel Multifunctional Ligands with μ/δ Opioid Agonist/Neurokinin-1 (NK1) Antagonist Activities for the Treatment of Pain.
Giri AK, Apostol CR, Wang Y, Forte BL, Largent-Milnes TM, Davis P, Rankin D, Molnar G, Olson KM, Porreca F, Vanderah TW, Hruby VJ.
J Med Chem (2015) 58 : 8573 -8583
PubMed 26465170 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.44 7.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4299483 1 7.58
CHEMBL4299390 1 7.57
CHEMBL4299423 1 7.54
CHEMBL438389 1 7.48
CHEMBL4299415 1 7.47
CHEMBL4299479 1 7.47
CHEMBL4299402 1 7.41
CHEMBL4299476 1 7.33
CHEMBL4299371 1 7.32
CHEMBL4299466 1 7.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4299483 Ki = 26.0 nM 7.58
CHEMBL4299390 Ki = 27.0 nM 7.57
CHEMBL4299423 Ki = 29.0 nM 7.54
CHEMBL438389 Ki = 33.0 nM 7.48
CHEMBL4299415 Ki = 34.0 nM 7.47
CHEMBL4299479 Ki = 34.0 nM 7.47
CHEMBL4299402 Ki = 39.0 nM 7.41
CHEMBL4299476 Ki = 47.0 nM 7.33
CHEMBL4299371 Ki = 48.0 nM 7.32
CHEMBL4299466 Ki = 61.0 nM 7.21