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Assay Detail

CHEMBL1810631

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Functional
Agonist activity at adrenergic beta1 receptor
26
Total Activities
26
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Beta-1 adrenergic receptor (CHEMBL213)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design-driven LO: the discovery of new ultra long acting dibasic β2-adrenoceptor agonists.
Connolly S, Alcaraz L, Bailey A, Cadogan E, Christie J, Cook AR, Fisher AJ, Hill S, Humphries A, Ingall AH, Kane Z, Paine S, Pairaudeau G, Stocks MJ, Young A.
Bioorg Med Chem Lett (2011) 21 : 4612 -4616
PubMed 21723724 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 7.16 8.40
pEC50 12 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1807819 1 8.40
CHEMBL1807832 1 7.50
CHEMBL1807872 1 7.40
CHEMBL1807870 1 7.40
CHEMBL1346 DARIFENACIN 4.0 1 7.40
CHEMBL1807830 1 7.40
CHEMBL1807871 1 7.20
CHEMBL1807829 1 7.00
CHEMBL1807827 1 7.00
CHEMBL1807828 1 7.00
CHEMBL1807869 1 7.00
CHEMBL1807873 1 6.80
CHEMBL1807874 1 6.70
CHEMBL1263 SALMETEROL 4.0 1 6.10
CHEMBL1256786 FORMOTEROL 4.0 1 -
CHEMBL82663 SIBENADET 2.0 1 -
CHEMBL1807817 1 -
CHEMBL1807818 1 -
CHEMBL1807820 1 -
CHEMBL1807821 1 -
CHEMBL1807822 1 -
CHEMBL1807823 1 -
CHEMBL1807824 1 -
CHEMBL1807825 1 -
CHEMBL1807826 1 -
CHEMBL1807831 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1807819 EC50 = 3.981 nM 8.40
CHEMBL1807832 EC50 = 31.62 nM 7.50
CHEMBL1807872 EC50 = 39.81 nM 7.40
CHEMBL1807870 EC50 = 39.81 nM 7.40
CHEMBL1346 DARIFENACIN EC50 = 39.81 nM 7.40
CHEMBL1807830 EC50 = 39.81 nM 7.40
CHEMBL1807871 EC50 = 63.1 nM 7.20
CHEMBL1807829 EC50 = 100.0 nM 7.00
CHEMBL1807827 EC50 = 100.0 nM 7.00
CHEMBL1807828 EC50 = 100.0 nM 7.00
CHEMBL1807869 EC50 = 100.0 nM 7.00
CHEMBL1807873 EC50 = 158.49 nM 6.80
CHEMBL1807874 EC50 = 199.53 nM 6.70
CHEMBL1263 SALMETEROL EC50 = 794.33 nM 6.10
CHEMBL1256786 FORMOTEROL pEC50 - -
CHEMBL82663 SIBENADET pEC50 - -
CHEMBL1807817 pEC50 - -
CHEMBL1807818 pEC50 - -
CHEMBL1807820 pEC50 - -
CHEMBL1807821 pEC50 - -
CHEMBL1807822 pEC50 - -
CHEMBL1807823 pEC50 - -
CHEMBL1807824 pEC50 - -
CHEMBL1807825 pEC50 - -
CHEMBL1807826 pEC50 - -
CHEMBL1807831 pEC50 - -