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Assay Detail

CHEMBL751789

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

Functional
In vitro functional activity towards Neurokinin NK2 receptor on isolated rabbit urinary bladder (RUB)
14
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Insertion of 2-carboxysuccinate and tricarballylic acid fragments into cyclic-pseudopeptides: new antagonists for the human tachykinin NK-2 receptor.
Harmat NJ, Giannotti D, Nannicini R, Perrotta E, Criscuoli M, Patacchini R, Renzetti AR, Giuliani S, Altamura M, Maggi CA.
Bioorg Med Chem Lett (2002) 12 : 693 -696
PubMed 11844703 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 14 8.61 9.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2112925 1 9.20
CHEMBL2112922 2 9.10
CHEMBL161242 1 9.00
CHEMBL2112923 1 9.00
CHEMBL159449 1 8.60
CHEMBL2112926 1 8.50
CHEMBL346285 1 8.50
CHEMBL345402 1 8.40
CHEMBL159585 1 8.40
CHEMBL435324 1 8.30
CHEMBL161288 1 8.20
CHEMBL2112924 1 8.20
CHEMBL350596 1 8.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2112925 Kd = 0.631 nM 9.20
CHEMBL2112922 Kd = 0.7943 nM 9.10
CHEMBL2112922 Kd = 0.7943 nM 9.10
CHEMBL161242 Kd = 1.0 nM 9.00
CHEMBL2112923 Kd = 1.0 nM 9.00
CHEMBL159449 Kd = 2.512 nM 8.60
CHEMBL2112926 Kd = 3.162 nM 8.50
CHEMBL346285 Kd = 3.162 nM 8.50
CHEMBL345402 Kd = 3.981 nM 8.40
CHEMBL159585 Kd = 3.981 nM 8.40
CHEMBL435324 Kd = 5.012 nM 8.30
CHEMBL161288 Kd = 6.31 nM 8.20
CHEMBL2112924 Kd = 6.31 nM 8.20
CHEMBL350596 Kd = 7.943 nM 8.10