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Assay Detail

CHEMBL3294890

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

Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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
Ki 29 6.24 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1263 SALMETEROL 4.0 1 8.60
CHEMBL1940832 MILVETEROL 2.0 1 8.50
CHEMBL1256786 FORMOTEROL 4.0 1 7.50
CHEMBL3290989 1 7.20
CHEMBL3290992 1 7.10
CHEMBL3290993 1 7.00
CHEMBL3290991 1 6.80
CHEMBL3290996 1 6.60
CHEMBL3290982 1 6.50
CHEMBL3290983 1 6.50
CHEMBL3290987 1 6.50
CHEMBL3290988 1 6.50
CHEMBL3290990 1 6.20
CHEMBL3290986 1 6.10
CHEMBL3290995 1 5.90
CHEMBL3290984 1 5.90
CHEMBL3290994 1 5.80
CHEMBL3290985 1 5.20
CHEMBL3290974 1 4.90
CHEMBL3290975 1 4.80
CHEMBL3290971 1 4.50
CHEMBL3290978 1 4.50
CHEMBL3290977 1 4.40
CHEMBL3290981 1 -
CHEMBL3290980 1 -
CHEMBL3290979 1 -
CHEMBL3290973 1 -
CHEMBL3290972 1 -
CHEMBL3290976 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1263 SALMETEROL Ki = 2.512 nM 8.60
CHEMBL1940832 MILVETEROL Ki = 3.162 nM 8.50
CHEMBL1256786 FORMOTEROL Ki = 31.62 nM 7.50
CHEMBL3290989 Ki = 63.1 nM 7.20
CHEMBL3290992 Ki = 79.43 nM 7.10
CHEMBL3290993 Ki = 100.0 nM 7.00
CHEMBL3290991 Ki = 158.49 nM 6.80
CHEMBL3290996 Ki = 251.19 nM 6.60
CHEMBL3290982 Ki = 316.23 nM 6.50
CHEMBL3290983 Ki = 316.23 nM 6.50
CHEMBL3290987 Ki = 316.23 nM 6.50
CHEMBL3290988 Ki = 316.23 nM 6.50
CHEMBL3290990 Ki = 630.96 nM 6.20
CHEMBL3290986 Ki = 794.33 nM 6.10
CHEMBL3290995 Ki = 1258.93 nM 5.90
CHEMBL3290984 Ki = 1258.93 nM 5.90
CHEMBL3290994 Ki = 1584.89 nM 5.80
CHEMBL3290985 Ki = 6309.57 nM 5.20
CHEMBL3290974 Ki = 12589.25 nM 4.90
CHEMBL3290975 Ki = 15848.93 nM 4.80
CHEMBL3290971 Ki = 31622.78 nM 4.50
CHEMBL3290978 Ki = 31622.78 nM 4.50
CHEMBL3290977 Ki = 39810.72 nM 4.40
CHEMBL3290981 Ki > 10000.0 nM -
CHEMBL3290980 Ki > 10000.0 nM -
CHEMBL3290979 Ki > 10000.0 nM -
CHEMBL3290973 Ki > 10000.0 nM -
CHEMBL3290972 Ki > 10000.0 nM -
CHEMBL3290976 Ki = 199526.23 nM -