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Assay Detail

CHEMBL816682

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

Binding
Competitive inhibition of [125I]NKA binding to hamster urinary bladder Tachykinin receptor 2
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cricetulus griseus
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Substance-K receptor (CHEMBL2304405)
Type SINGLE PROTEIN
Organism Mesocricetus auratus

Publication

A new class of high affinity ligands for the neurokinin A NK2 receptor: psi (CH2NR) reduced peptide bond analogues of neurokinin A4-10.
Harbeson SL, Shatzer SA, Le TB, Buck SH.
J Med Chem (1992) 35 : 3949 -3955
PubMed 1331450 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 7.24 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL339591 1 9.00
CHEMBL217406 NEUROKININ A 1 9.00
CHEMBL126294 1 8.22
CHEMBL340743 1 8.05
CHEMBL126776 1 8.00
CHEMBL437797 NEUROKININ B 1 7.75
CHEMBL339615 1 7.30
CHEMBL128854 1 6.99
CHEMBL340880 1 6.97
CHEMBL341015 1 6.94
CHEMBL341065 1 6.87
CHEMBL235363 SUBSTANCE P 1.0 1 6.83
CHEMBL129301 1 6.79
CHEMBL128521 1 6.71
CHEMBL336849 1 6.56
CHEMBL340847 1 5.78
CHEMBL339941 1 5.25
CHEMBL128175 1 -
CHEMBL409334 1 -
CHEMBL337970 1 -
CHEMBL262731 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL339591 IC50 = 1.0 nM 9.00
CHEMBL217406 NEUROKININ A IC50 = 1.0 nM 9.00
CHEMBL126294 IC50 = 6.0 nM 8.22
CHEMBL340743 IC50 = 9.0 nM 8.05
CHEMBL126776 IC50 = 10.0 nM 8.00
CHEMBL437797 NEUROKININ B IC50 = 18.0 nM 7.75
CHEMBL339615 IC50 = 50.0 nM 7.30
CHEMBL128854 IC50 = 103.0 nM 6.99
CHEMBL340880 IC50 = 108.0 nM 6.97
CHEMBL341015 IC50 = 115.0 nM 6.94
CHEMBL341065 IC50 = 136.0 nM 6.87
CHEMBL235363 SUBSTANCE P IC50 = 148.0 nM 6.83
CHEMBL129301 IC50 = 162.0 nM 6.79
CHEMBL128521 IC50 = 193.0 nM 6.71
CHEMBL336849 IC50 = 277.0 nM 6.56
CHEMBL340847 IC50 = 1652.0 nM 5.78
CHEMBL339941 IC50 = 5662.0 nM 5.25
CHEMBL128175 IC50 > 10000.0 nM -
CHEMBL409334 IC50 > 10000.0 nM -
CHEMBL337970 IC50 > 10000.0 nM -
CHEMBL262731 IC50 > 10000.0 nM -