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Assay Detail

CHEMBL3369039

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Functional
Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay
20
Total Activities
20
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of TD-4306, a long-acting β2-agonist for the treatment of asthma and COPD.
McKinnell RM, Klein U, Linsell MS, Moran EJ, Nodwell MB, Pfeiffer JW, Thomas GR, Yu C, Jacobsen JR.
Bioorg Med Chem Lett (2014) 24 : 2871 -2876
PubMed 24835980 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 19 7.53 8.20
pEC50 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3298324 1 8.20
CHEMBL3298987 1 8.10
CHEMBL3298326 1 8.00
CHEMBL3290999 1 7.90
CHEMBL3298762 1 7.90
CHEMBL3298692 1 7.90
CHEMBL1256786 FORMOTEROL 4.0 1 7.60
CHEMBL3298325 1 7.60
CHEMBL3298832 1 7.50
CHEMBL3298897 1 7.40
CHEMBL1940832 MILVETEROL 2.0 1 7.40
CHEMBL3298328 1 7.40
CHEMBL3298329 1 7.40
CHEMBL3298330 1 7.40
CHEMBL3298691 1 7.40
CHEMBL3298213 1 7.40
CHEMBL3298831 1 7.30
CHEMBL3298986 1 7.20
CHEMBL1263 SALMETEROL 4.0 1 6.00
CHEMBL3298327 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3298324 EC50 = 6.31 nM 8.20
CHEMBL3298987 EC50 = 7.943 nM 8.10
CHEMBL3298326 EC50 = 10.0 nM 8.00
CHEMBL3290999 EC50 = 12.59 nM 7.90
CHEMBL3298762 EC50 = 12.59 nM 7.90
CHEMBL3298692 EC50 = 12.59 nM 7.90
CHEMBL1256786 FORMOTEROL EC50 = 25.12 nM 7.60
CHEMBL3298325 EC50 = 25.12 nM 7.60
CHEMBL3298832 EC50 = 31.62 nM 7.50
CHEMBL3298897 EC50 = 39.81 nM 7.40
CHEMBL1940832 MILVETEROL EC50 = 39.81 nM 7.40
CHEMBL3298328 EC50 = 39.81 nM 7.40
CHEMBL3298329 EC50 = 39.81 nM 7.40
CHEMBL3298330 EC50 = 39.81 nM 7.40
CHEMBL3298691 EC50 = 39.81 nM 7.40
CHEMBL3298213 EC50 = 39.81 nM 7.40
CHEMBL3298831 EC50 = 50.12 nM 7.30
CHEMBL3298986 EC50 = 63.1 nM 7.20
CHEMBL1263 SALMETEROL EC50 = 1000.0 nM 6.00
CHEMBL3298327 pEC50 - -