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Assay Detail

CHEMBL1113306

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

Functional
Agonistic activity at human BRS3 expressed in HEK293AEO cells by aequorin bioluminescence assay
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Bombesin receptor subtype-3 (CHEMBL4080)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of substituted biphenyl imidazoles as potent, bioavailable bombesin receptor subtype-3 agonists.
He S, Dobbelaar PH, Liu J, Jian T, Sebhat IK, Lin LS, Goodman A, Guo C, Guzzo PR, Hadden M, Henderson AJ, Ruenz M, Sargent BJ, Yet L, Kelly TM, Palyha O, Kan Y, Pan J, Chen H, Marsh DJ, Shearman LP, Strack AM, Metzger JM, Feighner SD, Tan C, Howard AD, Tamvakopoulos C, Peng Q, Guan XM, Reitman ML, Patchett AA, Wyvratt MJ, Nargund RP.
Bioorg Med Chem Lett (2010) 20 : 1913 -1917
PubMed 20167483 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 43 6.13 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1089721 1 7.60
CHEMBL1089382 1 7.41
CHEMBL1099032 1 7.39
CHEMBL1093080 1 7.12
CHEMBL1084696 1 7.06
CHEMBL1099033 1 7.06
CHEMBL1089383 1 6.97
CHEMBL1091468 1 6.92
CHEMBL1082543 1 6.90
CHEMBL1084942 1 6.88
CHEMBL1088614 1 6.80
CHEMBL1088062 1 6.75
CHEMBL1085434 1 6.69
CHEMBL1080581 1 6.54
CHEMBL1097363 1 6.47
CHEMBL1097362 1 6.43
CHEMBL1084698 1 6.23
CHEMBL1099370 1 6.19
CHEMBL1082542 1 6.09
CHEMBL1086913 1 6.08
CHEMBL1084697 1 6.00
CHEMBL1077345 1 5.93
CHEMBL1085670 1 5.88
CHEMBL1086177 1 5.80
CHEMBL1083825 1 5.76
CHEMBL1079517 1 5.72
CHEMBL1087933 1 5.64
CHEMBL1086912 1 5.58
CHEMBL1079518 1 5.58
CHEMBL1079114 1 5.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1089721 EC50 = 25.0 nM 7.60
CHEMBL1089382 EC50 = 39.0 nM 7.41
CHEMBL1099032 EC50 = 41.0 nM 7.39
CHEMBL1093080 EC50 = 76.0 nM 7.12
CHEMBL1084696 EC50 = 87.0 nM 7.06
CHEMBL1099033 EC50 = 88.0 nM 7.06
CHEMBL1089383 EC50 = 106.0 nM 6.97
CHEMBL1091468 EC50 = 119.0 nM 6.92
CHEMBL1082543 EC50 = 127.0 nM 6.90
CHEMBL1084942 EC50 = 133.0 nM 6.88
CHEMBL1088614 EC50 = 159.0 nM 6.80
CHEMBL1088062 EC50 = 177.0 nM 6.75
CHEMBL1085434 EC50 = 205.0 nM 6.69
CHEMBL1080581 EC50 = 292.0 nM 6.54
CHEMBL1097363 EC50 = 338.0 nM 6.47
CHEMBL1097362 EC50 = 375.0 nM 6.43
CHEMBL1084698 EC50 = 588.0 nM 6.23
CHEMBL1099370 EC50 = 642.0 nM 6.19
CHEMBL1082542 EC50 = 812.0 nM 6.09
CHEMBL1086913 EC50 = 825.0 nM 6.08
CHEMBL1084697 EC50 = 1004.0 nM 6.00
CHEMBL1077345 EC50 = 1183.0 nM 5.93
CHEMBL1085670 EC50 = 1323.0 nM 5.88
CHEMBL1086177 EC50 = 1601.0 nM 5.80
CHEMBL1083825 EC50 = 1724.0 nM 5.76
CHEMBL1079517 EC50 = 1897.0 nM 5.72
CHEMBL1087933 EC50 = 2288.0 nM 5.64
CHEMBL1086912 EC50 = 2663.0 nM 5.58
CHEMBL1079518 EC50 = 2656.0 nM 5.58
CHEMBL1079114 EC50 = 2707.0 nM 5.57
CHEMBL1092798 EC50 = 2722.0 nM 5.57
CHEMBL1091087 EC50 = 2760.0 nM 5.56
CHEMBL1081130 EC50 = 4124.0 nM 5.38
CHEMBL1088468 EC50 = 4307.0 nM 5.37
CHEMBL1081866 EC50 = 4376.0 nM 5.36
CHEMBL1089720 EC50 = 4334.0 nM 5.36
CHEMBL1079696 EC50 = 4618.0 nM 5.34
CHEMBL1082041 EC50 = 4949.0 nM 5.30
CHEMBL1081131 EC50 = 5360.0 nM 5.27
CHEMBL1084130 EC50 = 5479.0 nM 5.26
CHEMBL1079869 EC50 = 5598.0 nM 5.25
CHEMBL1081132 EC50 = 5887.0 nM 5.23
CHEMBL1079697 EC50 > 10000.0 nM -