Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1111909

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

Functional
Agonist activity at rat BRS3 expressed in HEK293AEQ cells after 10 mins by aequorin bioluminescence assay
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Bombesin receptor subtype-3 (CHEMBL1075111)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis of 7-benzyl-5-(piperidin-1-yl)-6,7,8,9-tetrahydro-3H-pyrazolo[3,4-c][2,7]naphthyridin-1-ylamine and its analogs as bombesin receptor subtype-3 agonists.
Guo C, Guzzo PR, Hadden M, Sargent BJ, Yet L, Kan Y, Palyha O, Kelly TM, Guan X, Rosko K, Gagen K, Metzger JM, Dragovic J, Lyons K, Lin LS, Nargund RP.
Bioorg Med Chem Lett (2010) 20 : 2785 -2789
PubMed 20371178 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 36 5.83 7.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1098836 1 7.20
CHEMBL1096193 1 7.00
CHEMBL1099123 1 6.91
CHEMBL1099122 1 6.89
CHEMBL1099135 1 6.67
CHEMBL1098513 1 6.47
CHEMBL1098188 1 6.46
CHEMBL1095423 1 6.42
CHEMBL1096546 1 6.40
CHEMBL1098838 1 6.38
CHEMBL1098837 1 6.36
CHEMBL1095528 1 6.33
CHEMBL1098097 1 6.32
CHEMBL1095529 1 6.17
CHEMBL1097471 1 6.12
CHEMBL1094772 1 6.07
CHEMBL1095424 1 6.01
CHEMBL1096819 1 5.98
CHEMBL1095741 1 5.84
CHEMBL1098098 1 5.45
CHEMBL1199153 1 5.41
CHEMBL1095530 1 5.22
CHEMBL1097551 1 5.12
CHEMBL1098535 1 5.10
CHEMBL1094728 1 5.05
CHEMBL1098433 1 5.00
CHEMBL1094771 1 5.00
CHEMBL1094727 1 5.00
CHEMBL1098185 1 5.00
CHEMBL1098186 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1098836 EC50 = 63.0 nM 7.20
CHEMBL1096193 EC50 = 99.0 nM 7.00
CHEMBL1099123 EC50 = 123.0 nM 6.91
CHEMBL1099122 EC50 = 129.0 nM 6.89
CHEMBL1099135 EC50 = 212.0 nM 6.67
CHEMBL1098513 EC50 = 342.0 nM 6.47
CHEMBL1098188 EC50 = 346.0 nM 6.46
CHEMBL1095423 EC50 = 380.0 nM 6.42
CHEMBL1096546 EC50 = 402.0 nM 6.40
CHEMBL1098838 EC50 = 413.0 nM 6.38
CHEMBL1098837 EC50 = 433.0 nM 6.36
CHEMBL1095528 EC50 = 471.0 nM 6.33
CHEMBL1098097 EC50 = 481.0 nM 6.32
CHEMBL1095529 EC50 = 680.0 nM 6.17
CHEMBL1097471 EC50 = 759.0 nM 6.12
CHEMBL1094772 EC50 = 854.0 nM 6.07
CHEMBL1095424 EC50 = 965.0 nM 6.01
CHEMBL1096819 EC50 = 1057.0 nM 5.98
CHEMBL1095741 EC50 = 1442.0 nM 5.84
CHEMBL1098098 EC50 = 3557.0 nM 5.45
CHEMBL1199153 EC50 = 3859.0 nM 5.41
CHEMBL1095530 EC50 = 6056.0 nM 5.22
CHEMBL1097551 EC50 = 7652.0 nM 5.12
CHEMBL1098535 EC50 = 7906.0 nM 5.10
CHEMBL1094728 EC50 = 8954.0 nM 5.05
CHEMBL1094727 EC50 = 10000.0 nM 5.00
CHEMBL1096548 EC50 = 10000.0 nM 5.00
CHEMBL1096547 EC50 = 10000.0 nM 5.00
CHEMBL1096532 EC50 = 10000.0 nM 5.00
CHEMBL1096531 EC50 = 10000.0 nM 5.00
CHEMBL1098186 EC50 = 10000.0 nM 5.00
CHEMBL1098185 EC50 = 10000.0 nM 5.00
CHEMBL1094771 EC50 = 10000.0 nM 5.00
CHEMBL1098433 EC50 = 10000.0 nM 5.00
CHEMBL1204083 EC50 > 10000.0 nM -
CHEMBL1098825 EC50 > 10000.0 nM -