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Assay Detail

CHEMBL835446

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

Functional
pA2 for NK2 receptor of rabbit pulmonary artery
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Substance-K receptor (CHEMBL3433)
Type SINGLE PROTEIN
Organism Oryctolagus cuniculus

Publication

Structure-activity relationships of 1-alkyl-5-(3,4-dichlorophenyl)-5-{2-[3-(substituted)-1-azetidinyl]-ethyl}-2-piperidones. Part 2: Improving oral absorption.
Middleton DS, MacKenzie AR, Newman SD, Corless M, Warren A, Marchington AP, Jones B.
Bioorg Med Chem Lett (2005) 15 : 3957 -3961
PubMed 16039119 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 15 9.02 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL434548 1 10.10
CHEMBL367815 1 9.70
CHEMBL434142 1 9.70
CHEMBL360134 1 9.60
CHEMBL185572 1 9.00
CHEMBL185182 1 9.00
CHEMBL185007 1 8.90
CHEMBL365613 1 8.90
CHEMBL359655 1 8.90
CHEMBL185133 1 8.80
CHEMBL360721 1 8.70
CHEMBL367348 1 8.70
CHEMBL359903 1 8.60
CHEMBL185452 1 8.50
CHEMBL180049 1 8.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL434548 Kd = 0.07943 nM 10.10
CHEMBL367815 Kd = 0.1995 nM 9.70
CHEMBL434142 Kd = 0.1995 nM 9.70
CHEMBL360134 Kd = 0.2512 nM 9.60
CHEMBL185572 Kd = 1.0 nM 9.00
CHEMBL185182 Kd = 1.0 nM 9.00
CHEMBL185007 Kd = 1.259 nM 8.90
CHEMBL365613 Kd = 1.259 nM 8.90
CHEMBL359655 Kd = 1.259 nM 8.90
CHEMBL185133 Kd = 1.585 nM 8.80
CHEMBL360721 Kd = 1.995 nM 8.70
CHEMBL367348 Kd = 1.995 nM 8.70
CHEMBL359903 Kd = 2.512 nM 8.60
CHEMBL185452 Kd = 3.162 nM 8.50
CHEMBL180049 Kd = 6.31 nM 8.20