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Assay Detail

CHEMBL3129372

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

Binding
Displacement of [125I]-cyanopindolol from recombinant human beta-1 adrenergic receptor expressed in CHO cell membranes after 1 hr by scintillation counting analysis
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Beta-1 adrenergic receptor (CHEMBL213)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and evaluation of conformationally restricted acetanilides as potent and selective β3 adrenergic receptor agonists for the treatment of overactive bladder.
Moyes CR, Berger R, Goble SD, Harper B, Shen DM, Wang L, Bansal A, Brown PN, Chen AS, Dingley KH, Di Salvo J, Fitzmaurice A, Gichuru LN, Hurley AL, Jochnowitz N, Miller RR, Mistry S, Nagabukuro H, Salituro GM, Sanfiz A, Stevenson AS, Villa K, Zamlynny B, Struthers M, Weber AE, Edmondson SD.
J Med Chem (2014) 57 : 1437 -1453
PubMed 24437735 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 5.12 5.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3128184 1 5.36
CHEMBL3128185 1 4.88
CHEMBL3128187 1 -
CHEMBL3128186 1 -
CHEMBL3128183 1 -
CHEMBL3128182 1 -
CHEMBL3128181 1 -
CHEMBL3128180 1 -
CHEMBL3128179 1 -
CHEMBL3128178 1 -
CHEMBL3128177 1 -
CHEMBL3128201 1 -
CHEMBL3128200 1 -
CHEMBL3128199 1 -
CHEMBL3128188 1 -
CHEMBL3128197 1 -
CHEMBL3128196 1 -
CHEMBL3128195 1 -
CHEMBL3128194 1 -
CHEMBL3128193 1 -
CHEMBL3128192 1 -
CHEMBL3128191 1 -
CHEMBL3128190 1 -
CHEMBL3128189 1 -
CHEMBL1684585 1 -
CHEMBL3128198 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3128184 IC50 = 4329.0 nM 5.36
CHEMBL3128185 IC50 = 13340.0 nM 4.88
CHEMBL3128187 IC50 > 20000.0 nM -
CHEMBL3128186 IC50 > 20000.0 nM -
CHEMBL3128183 IC50 > 20000.0 nM -
CHEMBL3128182 IC50 > 20000.0 nM -
CHEMBL3128181 IC50 > 20000.0 nM -
CHEMBL3128180 IC50 > 20000.0 nM -
CHEMBL3128179 IC50 > 20000.0 nM -
CHEMBL3128178 IC50 > 20000.0 nM -
CHEMBL3128177 IC50 > 20000.0 nM -
CHEMBL3128201 IC50 > 20000.0 nM -
CHEMBL3128200 IC50 > 20000.0 nM -
CHEMBL3128199 IC50 > 20000.0 nM -
CHEMBL3128188 IC50 > 20000.0 nM -
CHEMBL3128197 IC50 > 20000.0 nM -
CHEMBL3128196 IC50 > 20000.0 nM -
CHEMBL3128195 IC50 > 20000.0 nM -
CHEMBL3128194 IC50 > 20000.0 nM -
CHEMBL3128193 IC50 > 20000.0 nM -
CHEMBL3128192 IC50 > 20000.0 nM -
CHEMBL3128191 IC50 > 20000.0 nM -
CHEMBL3128190 IC50 > 20000.0 nM -
CHEMBL3128189 IC50 > 20000.0 nM -
CHEMBL1684585 IC50 > 20000.0 nM -
CHEMBL3128198 IC50 > 20000.0 nM -