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Assay Detail

CHEMBL1261325

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Functional
Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL ↗
52
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Beta-3 adrenergic receptor (CHEMBL246) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Thienopyrimidines as β3-adrenoceptor agonists: hit-to-lead optimization.
Tasler S, Baumgartner R, Ammendola A, Schachtner J, Wieber T, Blisse M, Rath S, Zaja M, Klahn P, Quotschalla U, Ney P.
Bioorg Med Chem Lett (2010) 20 : 6108 -6115
PubMed 20833036 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 52 7.83 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1257555 — — 1 10.70
CHEMBL1257675 — — 1 10.40
CHEMBL1257797 — — 1 9.85
CHEMBL1258143 — — 1 9.30
CHEMBL1257913 — — 1 9.21
CHEMBL1258026 — — 1 9.00
CHEMBL1257438 — — 1 8.92
CHEMBL1257914 — — 1 8.80
CHEMBL1257554 — — 1 8.77
CHEMBL1258598 — — 1 8.77
CHEMBL1258707 — — 1 8.70
CHEMBL1257676 — — 1 8.66
CHEMBL1258023 — — 1 8.60
CHEMBL1258599 — — 1 8.55
CHEMBL1258485 — — 1 8.54
CHEMBL1258260 — — 1 8.51
CHEMBL1257916 — — 1 8.51
CHEMBL1258025 — — 1 8.33
CHEMBL1258372 — — 1 8.15
CHEMBL1258259 — — 1 8.11
CHEMBL1258257 — — 1 8.08
CHEMBL1257915 — — 1 8.00
CHEMBL1258486 — — 1 7.82
CHEMBL1255596 — — 1 7.75
CHEMBL1258373 — — 1 7.70
CHEMBL1258024 — — 1 7.68
CHEMBL1257674 — — 1 7.62
CHEMBL1258371 — — 1 7.58
CHEMBL1258706 — — 1 7.48
CHEMBL1258705 — — 1 7.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1257555 — EC50 = 0.02 nM 10.70
CHEMBL1257675 — EC50 = 0.04 nM 10.40
CHEMBL1257797 — EC50 = 0.14 nM 9.85
CHEMBL1258143 — EC50 = 0.5 nM 9.30
CHEMBL1257913 — EC50 = 0.62 nM 9.21
CHEMBL1258026 — EC50 = 1.0 nM 9.00
CHEMBL1257438 — EC50 = 1.2 nM 8.92
CHEMBL1257914 — EC50 = 1.6 nM 8.80
CHEMBL1257554 — EC50 = 1.7 nM 8.77
CHEMBL1258598 — EC50 = 1.7 nM 8.77
CHEMBL1258707 — EC50 = 2.0 nM 8.70
CHEMBL1257676 — EC50 = 2.2 nM 8.66
CHEMBL1258023 — EC50 = 2.5 nM 8.60
CHEMBL1258599 — EC50 = 2.8 nM 8.55
CHEMBL1258485 — EC50 = 2.9 nM 8.54
CHEMBL1258260 — EC50 = 3.1 nM 8.51
CHEMBL1257916 — EC50 = 3.1 nM 8.51
CHEMBL1258025 — EC50 = 4.7 nM 8.33
CHEMBL1258372 — EC50 = 7.1 nM 8.15
CHEMBL1258259 — EC50 = 7.8 nM 8.11
CHEMBL1258257 — EC50 = 8.3 nM 8.08
CHEMBL1257915 — EC50 = 10.0 nM 8.00
CHEMBL1258486 — EC50 = 15.0 nM 7.82
CHEMBL1255596 — EC50 = 18.0 nM 7.75
CHEMBL1258373 — EC50 = 20.0 nM 7.70
CHEMBL1258024 — EC50 = 21.0 nM 7.68
CHEMBL1257674 — EC50 = 24.0 nM 7.62
CHEMBL1258371 — EC50 = 26.0 nM 7.58
CHEMBL1258706 — EC50 = 33.0 nM 7.48
CHEMBL1258705 — EC50 = 35.0 nM 7.46
CHEMBL1258258 — EC50 = 41.0 nM 7.39
CHEMBL1257204 — EC50 = 55.0 nM 7.26
CHEMBL1258597 — EC50 = 79.0 nM 7.10
CHEMBL1258370 — EC50 = 92.0 nM 7.04
CHEMBL1258144 — EC50 = 96.0 nM 7.02
CHEMBL1257324 — EC50 = 97.0 nM 7.01
CHEMBL1258704 — EC50 = 100.0 nM 7.00
CHEMBL1258142 — EC50 = 113.0 nM 6.95
CHEMBL1083995 — EC50 = 120.0 nM 6.92
CHEMBL1258827 — EC50 = 150.0 nM 6.82
CHEMBL1257796 — EC50 = 150.0 nM 6.82
CHEMBL1258826 — EC50 = 150.0 nM 6.82
CHEMBL1256008 — EC50 = 150.0 nM 6.82
CHEMBL1257205 — EC50 = 150.0 nM 6.82
CHEMBL1257206 — EC50 = 150.0 nM 6.82
CHEMBL1258942 — EC50 = 150.0 nM 6.82
CHEMBL1258941 — EC50 = 150.0 nM 6.82
CHEMBL1258824 — EC50 = 150.0 nM 6.82
CHEMBL1258484 — EC50 = 264.0 nM 6.58
CHEMBL1257798 — EC50 = 310.0 nM 6.51