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Assay Detail

CHEMBL4427988

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

Binding
Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Bombesin receptor subtype-3 (CHEMBL1075140)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Synthesis and biological evaluation of novel imidazol-1-ylacetic acid derivatives as non-brain penetrant bombesin receptor subtype-3 (BRS-3) agonists.
Kiyotsuka Y, Shimada K, Kobayashi S, Suzuki M, Akiu M, Asano M, Sogawa Y, Hara T, Konishi M, Abe-Ohya R, Izumi M, Nagai Y, Yoshida K, Abe Y, Takamori H, Takahashi H.
Bioorg Med Chem Lett (2016) 26 : 4205 -4210
PubMed 27491709 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 7.29 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4435571 1 9.10
CHEMBL4580739 1 8.70
CHEMBL4461212 1 8.52
CHEMBL4448589 1 8.40
CHEMBL4593256 1 8.30
CHEMBL4464287 1 8.15
CHEMBL4522752 1 7.89
CHEMBL4482945 1 7.62
CHEMBL4557722 1 7.60
CHEMBL4449347 1 7.58
CHEMBL4514194 1 7.36
CHEMBL4451347 1 7.21
CHEMBL4476111 1 6.85
CHEMBL4544477 1 6.30
CHEMBL4442362 1 6.21
CHEMBL4522974 1 6.16
CHEMBL4590481 1 5.90
CHEMBL4518142 1 5.72
CHEMBL4448645 1 5.00
CHEMBL4585527 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4435571 EC50 = 0.8 nM 9.10
CHEMBL4580739 EC50 = 2.0 nM 8.70
CHEMBL4461212 EC50 = 3.0 nM 8.52
CHEMBL4448589 EC50 = 4.0 nM 8.40
CHEMBL4593256 EC50 = 5.0 nM 8.30
CHEMBL4464287 EC50 = 7.0 nM 8.15
CHEMBL4522752 EC50 = 13.0 nM 7.89
CHEMBL4482945 EC50 = 24.0 nM 7.62
CHEMBL4557722 EC50 = 25.0 nM 7.60
CHEMBL4449347 EC50 = 26.0 nM 7.58
CHEMBL4514194 EC50 = 44.0 nM 7.36
CHEMBL4451347 EC50 = 61.0 nM 7.21
CHEMBL4476111 EC50 = 140.0 nM 6.85
CHEMBL4544477 EC50 = 498.0 nM 6.30
CHEMBL4442362 EC50 = 621.0 nM 6.21
CHEMBL4522974 EC50 = 694.0 nM 6.16
CHEMBL4590481 EC50 = 1271.0 nM 5.90
CHEMBL4518142 EC50 = 1906.0 nM 5.72
CHEMBL4448645 EC50 = 9908.0 nM 5.00
CHEMBL4585527 EC50 > 10000.0 nM -