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Assay Detail

CHEMBL1105983

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

Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL ↗
59
Total Activities
59
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-2 adrenergic receptor (CHEMBL210) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Heterocyclic acetamide and benzamide derivatives as potent and selective beta3-adrenergic receptor agonists with improved rodent pharmacokinetic profiles.
Goble SD, Wang L, Howell KL, Bansal A, Berger R, Brockunier L, DiSalvo J, Feighner S, Harper B, He J, Hurley A, Hreniuk D, Parmee E, Robbins M, Salituro G, Sanfiz A, Streckfuss E, Watkins E, Weber AE, Struthers M, Edmondson SD.
Bioorg Med Chem Lett (2010) 20 : 1895 -1899
PubMed 20181479 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 59 5.64 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1089734 — — 1 7.22
CHEMBL1078695 — — 1 7.00
CHEMBL1089396 — — 1 6.40
CHEMBL1078749 — — 1 6.40
CHEMBL1078576 — — 1 6.40
CHEMBL1077273 — — 1 6.22
CHEMBL1078496 — — 1 6.22
CHEMBL1085693 — — 1 5.96
CHEMBL1089725 — — 1 5.96
CHEMBL1078465 — — 1 5.77
CHEMBL1084137 — — 1 5.77
CHEMBL1090746 — — 1 5.77
CHEMBL111201 — — 1 5.64
CHEMBL1083832 — — 1 5.52
CHEMBL1083216 — — 1 5.44
CHEMBL1078495 — — 1 5.33
CHEMBL1089735 — — 1 5.28
CHEMBL1086149 — — 1 5.22
CHEMBL1085444 — — 1 5.17
CHEMBL1078395 — — 1 5.16
CHEMBL1084145 — — 1 5.11
CHEMBL1090425 — — 1 5.06
CHEMBL1089387 — — 1 4.89
CHEMBL1078696 — — 1 4.82
CHEMBL1092502 — — 1 4.82
CHEMBL1078876 — — 1 4.80
CHEMBL1089052 — — 1 4.80
CHEMBL1089395 — — 1 -
CHEMBL1089053 — — 1 -
CHEMBL1091816 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1089734 — IC50 = 60.0 nM 7.22
CHEMBL1078695 — IC50 = 100.0 nM 7.00
CHEMBL1078749 — IC50 = 400.0 nM 6.40
CHEMBL1078576 — IC50 = 400.0 nM 6.40
CHEMBL1089396 — IC50 = 400.0 nM 6.40
CHEMBL1077273 — IC50 = 600.0 nM 6.22
CHEMBL1078496 — IC50 = 600.0 nM 6.22
CHEMBL1085693 — IC50 = 1100.0 nM 5.96
CHEMBL1089725 — IC50 = 1100.0 nM 5.96
CHEMBL1078465 — IC50 = 1700.0 nM 5.77
CHEMBL1084137 — IC50 = 1700.0 nM 5.77
CHEMBL1090746 — IC50 = 1700.0 nM 5.77
CHEMBL111201 — IC50 = 2300.0 nM 5.64
CHEMBL1083832 — IC50 = 3000.0 nM 5.52
CHEMBL1083216 — IC50 = 3600.0 nM 5.44
CHEMBL1078495 — IC50 = 4700.0 nM 5.33
CHEMBL1089735 — IC50 = 5300.0 nM 5.28
CHEMBL1086149 — IC50 = 6000.0 nM 5.22
CHEMBL1085444 — IC50 = 6700.0 nM 5.17
CHEMBL1078395 — IC50 = 6900.0 nM 5.16
CHEMBL1084145 — IC50 = 7800.0 nM 5.11
CHEMBL1090425 — IC50 = 8700.0 nM 5.06
CHEMBL1089387 — IC50 = 13000.0 nM 4.89
CHEMBL1078696 — IC50 = 15000.0 nM 4.82
CHEMBL1092502 — IC50 = 15000.0 nM 4.82
CHEMBL1078876 — IC50 = 16000.0 nM 4.80
CHEMBL1089052 — IC50 = 16000.0 nM 4.80
CHEMBL1085897 — IC50 > 20000.0 nM -
CHEMBL1084144 — IC50 > 10000.0 nM -
CHEMBL1091479 — IC50 > 20000.0 nM -
CHEMBL1086411 — IC50 > 20000.0 nM -
CHEMBL1084138 — IC50 > 10000.0 nM -
CHEMBL1084136 — IC50 > 10000.0 nM -
CHEMBL1090424 — IC50 > 10000.0 nM -
CHEMBL1093387 — IC50 > 20000.0 nM -
CHEMBL1093086 — IC50 > 20000.0 nM -
CHEMBL1089386 — IC50 > 10000.0 nM -
CHEMBL1084667 — IC50 > 10000.0 nM -
CHEMBL1085898 — IC50 > 10000.0 nM -
CHEMBL1077199 — IC50 > 20000.0 nM -
CHEMBL1077238 — IC50 > 10000.0 nM -
CHEMBL1078575 — IC50 > 10000.0 nM -
CHEMBL1078394 — IC50 > 20000.0 nM -
CHEMBL1083831 — IC50 > 20000.0 nM -
CHEMBL1085442 — IC50 > 10000.0 nM -
CHEMBL1085441 — IC50 > 10000.0 nM -
CHEMBL1094715 — IC50 > 20000.0 nM -
CHEMBL1091816 — IC50 > 20000.0 nM -
CHEMBL1089053 — IC50 > 20000.0 nM -
CHEMBL1089395 — IC50 > 20000.0 nM -