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Assay Detail

CHEMBL857059

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Binding
Inhibitory activity against human Tachykinin receptor 2
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Substance-K receptor (CHEMBL2327)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Importance of the aromatic residue at position 6 of [Nle(10)]neurokinin A(4-10) for binding to the NK-2 receptor and receptor activation.
Gembitsky DS, Murnin M, Otvös FL, Allen J, Murphy RF, Lovas S.
J Med Chem (1999) 42 : 3004 -3007
PubMed 10425111 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.96 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL217406 NEUROKININ A 1 8.77
CHEMBL431641 1 7.51
CHEMBL437797 NEUROKININ B 1 6.99
CHEMBL103634 1 6.97
CHEMBL235363 SUBSTANCE P 1.0 1 6.61
CHEMBL103939 1 6.43
CHEMBL102128 1 5.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL217406 NEUROKININ A IC50 = 1.698 nM 8.77
CHEMBL431641 IC50 = 30.9 nM 7.51
CHEMBL437797 NEUROKININ B IC50 = 102.33 nM 6.99
CHEMBL103634 IC50 = 107.15 nM 6.97
CHEMBL235363 SUBSTANCE P IC50 = 245.47 nM 6.61
CHEMBL103939 IC50 = 371.54 nM 6.43
CHEMBL102128 IC50 = 3467.37 nM 5.46