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Assay Detail

CHEMBL3294889

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Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
32
Total Activities
32
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

Beta-2 adrenergic receptor (CHEMBL210)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Multivalent design of long-acting β(2)-adrenoceptor agonists incorporating biarylamines.
Jacobsen JR, Aggen JB, Church TJ, Klein U, Pfeiffer JW, Pulido-Rios TM, Thomas GR, Yu C, Moran EJ.
Bioorg Med Chem Lett (2014) 24 : 2625 -2630
PubMed 24813741 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 32 7.77 10.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1940832 MILVETEROL 2.0 1 10.20
CHEMBL3290999 1 9.90
CHEMBL3290998 1 9.90
CHEMBL1256786 FORMOTEROL 4.0 1 9.70
CHEMBL1263 SALMETEROL 4.0 1 9.50
CHEMBL3290997 1 9.30
CHEMBL3290991 1 8.90
CHEMBL3290989 1 8.90
CHEMBL3290988 1 8.70
CHEMBL3290993 1 8.60
CHEMBL3290992 1 8.60
CHEMBL3290983 1 8.60
CHEMBL3290984 1 8.40
CHEMBL3290996 1 8.20
CHEMBL3290987 1 8.10
CHEMBL3290986 1 8.10
CHEMBL3290990 1 8.00
CHEMBL3290982 1 7.70
CHEMBL3290971 1 7.60
CHEMBL3290995 1 7.50
CHEMBL3290973 1 6.80
CHEMBL3290985 1 6.70
CHEMBL3290978 1 6.70
CHEMBL3290994 1 6.70
CHEMBL3290974 1 6.40
CHEMBL3290975 1 6.30
CHEMBL3290979 1 6.20
CHEMBL3290981 1 6.00
CHEMBL3290977 1 5.90
CHEMBL3290972 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1940832 MILVETEROL EC50 = 0.0631 nM 10.20
CHEMBL3290999 EC50 = 0.1259 nM 9.90
CHEMBL3290998 EC50 = 0.1259 nM 9.90
CHEMBL1256786 FORMOTEROL EC50 = 0.1995 nM 9.70
CHEMBL1263 SALMETEROL EC50 = 0.3162 nM 9.50
CHEMBL3290997 EC50 = 0.5012 nM 9.30
CHEMBL3290991 EC50 = 1.259 nM 8.90
CHEMBL3290989 EC50 = 1.259 nM 8.90
CHEMBL3290988 EC50 = 1.995 nM 8.70
CHEMBL3290993 EC50 = 2.512 nM 8.60
CHEMBL3290992 EC50 = 2.512 nM 8.60
CHEMBL3290983 EC50 = 2.512 nM 8.60
CHEMBL3290984 EC50 = 3.981 nM 8.40
CHEMBL3290996 EC50 = 6.31 nM 8.20
CHEMBL3290986 EC50 = 7.943 nM 8.10
CHEMBL3290987 EC50 = 7.943 nM 8.10
CHEMBL3290990 EC50 = 10.0 nM 8.00
CHEMBL3290982 EC50 = 19.95 nM 7.70
CHEMBL3290971 EC50 = 25.12 nM 7.60
CHEMBL3290995 EC50 = 31.62 nM 7.50
CHEMBL3290973 EC50 = 158.49 nM 6.80
CHEMBL3290985 EC50 = 199.53 nM 6.70
CHEMBL3290978 EC50 = 199.53 nM 6.70
CHEMBL3290994 EC50 = 199.53 nM 6.70
CHEMBL3290974 EC50 = 398.11 nM 6.40
CHEMBL3290975 EC50 = 501.19 nM 6.30
CHEMBL3290979 EC50 = 630.96 nM 6.20
CHEMBL3290981 EC50 = 1000.0 nM 6.00
CHEMBL3290977 EC50 = 1258.93 nM 5.90
CHEMBL3290972 EC50 = 1584.89 nM 5.80
CHEMBL3290976 EC50 = 1584.89 nM 5.80
CHEMBL3290980 EC50 = 10000.0 nM 5.00