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Assay Detail

CHEMBL817325

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Binding
The compound was tested for competition binding with [3H]NKA against the CHO cells from cloned human Tachykinin receptor 2
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
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
Ki 9 7.35 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL217406 NEUROKININ A 1 9.15
CHEMBL431641 1 7.90
CHEMBL437797 NEUROKININ B 1 7.38
CHEMBL103634 1 7.36
CHEMBL235363 SUBSTANCE P 1.0 1 6.99
CHEMBL103939 1 6.81
CHEMBL102128 1 5.85
CHEMBL319256 1 -
CHEMBL430650 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL217406 NEUROKININ A Ki = 0.71 nM 9.15
CHEMBL431641 Ki = 12.7 nM 7.90
CHEMBL437797 NEUROKININ B Ki = 42.2 nM 7.38
CHEMBL103634 Ki = 44.2 nM 7.36
CHEMBL235363 SUBSTANCE P Ki = 102.0 nM 6.99
CHEMBL103939 Ki = 156.0 nM 6.81
CHEMBL102128 Ki = 1422.0 nM 5.85
CHEMBL319256 Ki > 2000.0 nM -
CHEMBL430650 Ki > 2000.0 nM -