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Assay Detail

CHEMBL1947791

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

Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL ↗
52
Total Activities
52
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

From libraries to candidate: the discovery of new ultra long-acting dibasic β₂-adrenoceptor agonists.
Alcaraz L, Bailey A, Cadogan E, Connolly S, Jewell R, Jordan S, Kindon N, Lister A, Lawson M, Mullen A, Dainty I, Nicholls D, Paine S, Pairaudeau G, Stocks MJ, Thorne P, Young A.
Bioorg Med Chem Lett (2012) 22 : 689 -695
PubMed 22079756 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 50 8.06 9.70
pIC50 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1945036 — — 1 9.70
CHEMBL1947157 — — 1 9.70
CHEMBL1944691 — — 1 9.30
CHEMBL1945038 — — 1 9.30
CHEMBL1944690 — — 1 9.20
CHEMBL1946768 — — 1 9.20
CHEMBL1945031 — — 1 9.20
CHEMBL1947151 — — 1 9.10
CHEMBL1945037 — — 1 9.10
CHEMBL1944693 — — 1 9.10
CHEMBL1945042 — — 1 9.00
CHEMBL1945299 — — 1 8.80
CHEMBL1947155 — — 1 8.70
CHEMBL1945032 — — 1 8.70
CHEMBL1944692 — — 1 8.70
CHEMBL1944695 — — 1 8.70
CHEMBL1944694 — — 1 8.70
CHEMBL1945041 — — 1 8.70
CHEMBL1945033 — — 1 8.60
CHEMBL1945034 — — 1 8.50
CHEMBL1944689 — — 1 8.40
CHEMBL1947153 — — 1 8.40
CHEMBL1945294 — — 1 8.40
CHEMBL1945289 — — 1 8.30
CHEMBL1945039 — — 1 8.20
CHEMBL1945044 — — 1 8.20
CHEMBL1945296 — — 1 8.20
CHEMBL1945298 — — 1 8.10
CHEMBL1947156 — — 1 8.00
CHEMBL1945035 — — 1 7.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1945036 — IC50 = 0.1995 nM 9.70
CHEMBL1947157 — IC50 = 0.1995 nM 9.70
CHEMBL1945038 — IC50 = 0.5012 nM 9.30
CHEMBL1944691 — IC50 = 0.5012 nM 9.30
CHEMBL1944690 — IC50 = 0.631 nM 9.20
CHEMBL1946768 — IC50 = 0.631 nM 9.20
CHEMBL1945031 — IC50 = 0.631 nM 9.20
CHEMBL1947151 — IC50 = 0.7943 nM 9.10
CHEMBL1945037 — IC50 = 0.7943 nM 9.10
CHEMBL1944693 — IC50 = 0.7943 nM 9.10
CHEMBL1945042 — IC50 = 1.0 nM 9.00
CHEMBL1945299 — IC50 = 1.585 nM 8.80
CHEMBL1944695 — IC50 = 1.995 nM 8.70
CHEMBL1945032 — IC50 = 1.995 nM 8.70
CHEMBL1944692 — IC50 = 1.995 nM 8.70
CHEMBL1947155 — IC50 = 1.995 nM 8.70
CHEMBL1944694 — IC50 = 1.995 nM 8.70
CHEMBL1945041 — IC50 = 1.995 nM 8.70
CHEMBL1945033 — IC50 = 2.512 nM 8.60
CHEMBL1945034 — IC50 = 3.162 nM 8.50
CHEMBL1944689 — IC50 = 3.981 nM 8.40
CHEMBL1947153 — IC50 = 3.981 nM 8.40
CHEMBL1945294 — IC50 = 3.981 nM 8.40
CHEMBL1945289 — IC50 = 5.012 nM 8.30
CHEMBL1945296 — IC50 = 6.31 nM 8.20
CHEMBL1945044 — IC50 = 6.31 nM 8.20
CHEMBL1945039 — IC50 = 6.31 nM 8.20
CHEMBL1945298 — IC50 = 7.943 nM 8.10
CHEMBL1947156 — IC50 = 10.0 nM 8.00
CHEMBL1945035 — IC50 = 12.59 nM 7.90
CHEMBL1946765 — IC50 = 12.59 nM 7.90
CHEMBL1945043 — IC50 = 15.85 nM 7.80
CHEMBL1947150 — IC50 = 15.85 nM 7.80
CHEMBL1945290 — IC50 = 25.12 nM 7.60
CHEMBL1945291 — IC50 = 25.12 nM 7.60
CHEMBL1945292 — IC50 = 25.12 nM 7.60
CHEMBL1946769 — IC50 = 31.62 nM 7.50
CHEMBL1947152 — IC50 = 31.62 nM 7.50
CHEMBL1947154 — IC50 = 63.1 nM 7.20
CHEMBL1945503 — IC50 = 63.1 nM 7.20
CHEMBL1946763 — IC50 = 100.0 nM 7.00
CHEMBL1945040 — IC50 = 125.89 nM 6.90
CHEMBL1946764 — IC50 = 125.89 nM 6.90
CHEMBL1946767 — IC50 = 199.53 nM 6.70
CHEMBL1945504 — IC50 = 251.19 nM 6.60
CHEMBL1945293 — IC50 = 316.23 nM 6.50
CHEMBL1946761 — IC50 = 501.19 nM 6.30
CHEMBL1945300 — IC50 = 630.96 nM 6.20
CHEMBL1946766 — IC50 = 794.33 nM 6.10
CHEMBL1946762 — IC50 = 1258.93 nM 5.90