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Assay Detail

CHEMBL647875

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

Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Potent, selective 3-pyridylethanolamine beta3 adrenergic receptor agonists possessing a thiazole benzenesulfonamide pharmacophore.
Mathvink RJ, Tolman JS, Chitty D, Candelore MR, Cascieri MA, Colwell LF, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Tota L, Wyvratt MJ, Fisher MH, Weber AE.
Bioorg Med Chem Lett (2000) 10 : 1971 -1973
PubMed 10987429 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 5.28 6.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL291992 1 6.21
CHEMBL59270 1 6.04
CHEMBL291593 1 6.00
CHEMBL293994 1 5.77
CHEMBL58798 1 5.72
CHEMBL294753 1 5.70
CHEMBL61429 1 5.70
CHEMBL291594 1 5.68
CHEMBL418308 1 5.64
CHEMBL430594 1 5.60
CHEMBL60281 1 5.52
CHEMBL294492 1 5.52
CHEMBL294172 1 5.52
CHEMBL433248 1 5.40
CHEMBL61962 1 5.24
CHEMBL58407 1 5.20
CHEMBL292598 1 5.10
CHEMBL294849 1 4.80
CHEMBL293577 1 4.33
CHEMBL57908 1 4.31
CHEMBL291516 1 4.30
CHEMBL58241 1 4.05
CHEMBL291306 1 4.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL291992 IC50 = 620.0 nM 6.21
CHEMBL59270 IC50 = 910.0 nM 6.04
CHEMBL291593 IC50 = 1000.0 nM 6.00
CHEMBL293994 IC50 = 1700.0 nM 5.77
CHEMBL58798 IC50 = 1900.0 nM 5.72
CHEMBL294753 IC50 = 2000.0 nM 5.70
CHEMBL61429 IC50 = 2000.0 nM 5.70
CHEMBL291594 IC50 = 2100.0 nM 5.68
CHEMBL418308 IC50 = 2300.0 nM 5.64
CHEMBL430594 IC50 = 2500.0 nM 5.60
CHEMBL60281 IC50 = 3000.0 nM 5.52
CHEMBL294492 IC50 = 3000.0 nM 5.52
CHEMBL294172 IC50 = 3000.0 nM 5.52
CHEMBL433248 IC50 = 4000.0 nM 5.40
CHEMBL61962 IC50 = 5700.0 nM 5.24
CHEMBL58407 IC50 = 6300.0 nM 5.20
CHEMBL292598 IC50 = 8000.0 nM 5.10
CHEMBL294849 IC50 = 16000.0 nM 4.80
CHEMBL293577 IC50 = 47000.0 nM 4.33
CHEMBL57908 IC50 = 49000.0 nM 4.31
CHEMBL291516 IC50 = 50000.0 nM 4.30
CHEMBL58241 IC50 = 90000.0 nM 4.05
CHEMBL291306 IC50 = 93000.0 nM 4.03