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Assay Detail

CHEMBL4375060

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Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL ↗
41
Total Activities
18
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Probing the Existence of a Metastable Binding Site at the β<sub>2</sub>-Adrenergic Receptor with Homobivalent Bitopic Ligands.
Gaiser BI, Danielsen M, Marcher-Rørsted E, Røpke Jørgensen K, Wróbel TM, Frykman M, Johansson H, Bräuner-Osborne H, Gloriam DE, Mathiesen JM, Sejer Pedersen D.
J Med Chem (2019) 62 : 7806 -7839
PubMed 31298548 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 8.57 9.42
Inhibition 17 - -
Kd 6 9.01 9.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL723 CARVEDILOL 4.0 1 9.71
CHEMBL4564189 — — 2 9.42
CHEMBL4514723 — — 2 9.36
CHEMBL4594173 — — 3 9.12
CHEMBL4527821 — — 2 9.10
CHEMBL1160734 — — 3 9.05
CHEMBL4462252 — — 2 9.05
CHEMBL4473518 — — 2 9.02
CHEMBL4441975 — — 2 8.94
CHEMBL4446394 — — 3 8.93
CHEMBL266195 ALPRENOLOL 2.0 5 8.92
CHEMBL4434772 — — 2 8.82
CHEMBL4574652 — — 2 8.46
CHEMBL4450606 — — 2 7.93
CHEMBL4442559 — — 2 7.81
CHEMBL1395661 — — 2 7.74
CHEMBL4530266 — — 2 7.41
CHEMBL4474813 — — 2 6.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL723 CARVEDILOL Kd = 0.195 nM 9.71
CHEMBL4564189 — Ki = 0.3802 nM 9.42
CHEMBL4514723 — Ki = 0.4365 nM 9.36
CHEMBL4594173 — Ki = 0.7586 nM 9.12
CHEMBL4527821 — Ki = 0.7943 nM 9.10
CHEMBL1160734 — Kd = 0.8913 nM 9.05
CHEMBL4462252 — Ki = 0.8913 nM 9.05
CHEMBL1160734 — Ki = 0.9333 nM 9.03
CHEMBL4473518 — Ki = 0.955 nM 9.02
CHEMBL4441975 — Ki = 1.148 nM 8.94
CHEMBL4446394 — Ki = 1.175 nM 8.93
CHEMBL266195 ALPRENOLOL Ki = 1.2 nM 8.92
CHEMBL266195 ALPRENOLOL Ki = 1.202 nM 8.92
CHEMBL4594173 — Kd = 1.288 nM 8.89
CHEMBL266195 ALPRENOLOL Kd = 1.45 nM 8.84
CHEMBL266195 ALPRENOLOL Kd = 1.445 nM 8.84
CHEMBL4434772 — Ki = 1.514 nM 8.82
CHEMBL4446394 — Kd = 1.905 nM 8.72
CHEMBL4574652 — Ki = 3.467 nM 8.46
CHEMBL4450606 — Ki = 11.75 nM 7.93
CHEMBL4442559 — Ki = 15.49 nM 7.81
CHEMBL1395661 — Ki = 18.2 nM 7.74
CHEMBL4530266 — Ki = 38.9 nM 7.41
CHEMBL4474813 — Ki = 467.74 nM 6.33
CHEMBL1160734 — Inhibition - % -
CHEMBL1395661 — Inhibition - % -
CHEMBL266195 ALPRENOLOL Inhibition - % -
CHEMBL4473518 — Inhibition - % -
CHEMBL4527821 — Inhibition - % -
CHEMBL4434772 — Inhibition - % -
CHEMBL4441975 — Inhibition - % -
CHEMBL4574652 — Inhibition - % -
CHEMBL4446394 — Inhibition - % -
CHEMBL4564189 — Inhibition - % -
CHEMBL4474813 — Inhibition - % -
CHEMBL4450606 — Inhibition - % -
CHEMBL4594173 — Inhibition - % -
CHEMBL4530266 — Inhibition - % -
CHEMBL4442559 — Inhibition - % -
CHEMBL4462252 — Inhibition - % -
CHEMBL4514723 — Inhibition - % -