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Assay Detail

CHEMBL1947789

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Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL ↗
50
Total Activities
50
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type H292
Confidence 9 — Direct 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
EC50 50 8.74 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1944691 — — 1 9.80
CHEMBL1945034 — — 1 9.70
CHEMBL1945032 — — 1 9.60
CHEMBL1944695 — — 1 9.60
CHEMBL1944690 — — 1 9.60
CHEMBL1945031 — — 1 9.50
CHEMBL1944694 — — 1 9.50
CHEMBL1945041 — — 1 9.50
CHEMBL1944693 — — 1 9.50
CHEMBL1944689 — — 1 9.50
CHEMBL1945299 — — 1 9.40
CHEMBL1945036 — — 1 9.40
CHEMBL1944692 — — 1 9.40
CHEMBL1947157 — — 1 9.30
CHEMBL1945037 — — 1 9.30
CHEMBL1945033 — — 1 9.30
CHEMBL1947156 — — 1 9.20
CHEMBL1945039 — — 1 9.20
CHEMBL1945042 — — 1 9.20
CHEMBL1945043 — — 1 9.20
CHEMBL1945294 — — 1 9.20
CHEMBL82663 SIBENADET 2.0 1 9.20
CHEMBL1263 SALMETEROL 4.0 1 9.10
CHEMBL1945289 — — 1 9.10
CHEMBL1945297 — — 1 9.10
CHEMBL1256786 FORMOTEROL 4.0 1 9.00
CHEMBL1945038 — — 1 9.00
CHEMBL1947153 — — 1 9.00
CHEMBL1945044 — — 1 9.00
CHEMBL1945296 — — 1 8.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1944691 — EC50 = 0.1585 nM 9.80
CHEMBL1945034 — EC50 = 0.1995 nM 9.70
CHEMBL1945032 — EC50 = 0.2512 nM 9.60
CHEMBL1944695 — EC50 = 0.2512 nM 9.60
CHEMBL1944690 — EC50 = 0.2512 nM 9.60
CHEMBL1945031 — EC50 = 0.3162 nM 9.50
CHEMBL1944694 — EC50 = 0.3162 nM 9.50
CHEMBL1945041 — EC50 = 0.3162 nM 9.50
CHEMBL1944693 — EC50 = 0.3162 nM 9.50
CHEMBL1944689 — EC50 = 0.3162 nM 9.50
CHEMBL1945299 — EC50 = 0.3981 nM 9.40
CHEMBL1945036 — EC50 = 0.3981 nM 9.40
CHEMBL1944692 — EC50 = 0.3981 nM 9.40
CHEMBL1945033 — EC50 = 0.5012 nM 9.30
CHEMBL1947157 — EC50 = 0.5012 nM 9.30
CHEMBL1945037 — EC50 = 0.5012 nM 9.30
CHEMBL1947156 — EC50 = 0.631 nM 9.20
CHEMBL1945039 — EC50 = 0.631 nM 9.20
CHEMBL1945042 — EC50 = 0.631 nM 9.20
CHEMBL1945043 — EC50 = 0.631 nM 9.20
CHEMBL1945294 — EC50 = 0.631 nM 9.20
CHEMBL82663 SIBENADET EC50 = 0.631 nM 9.20
CHEMBL1263 SALMETEROL EC50 = 0.7943 nM 9.10
CHEMBL1945289 — EC50 = 0.7943 nM 9.10
CHEMBL1945297 — EC50 = 0.7943 nM 9.10
CHEMBL1256786 FORMOTEROL EC50 = 1.0 nM 9.00
CHEMBL1945044 — EC50 = 1.0 nM 9.00
CHEMBL1945038 — EC50 = 1.0 nM 9.00
CHEMBL1947153 — EC50 = 1.0 nM 9.00
CHEMBL1945296 — EC50 = 1.259 nM 8.90
CHEMBL1945035 — EC50 = 1.585 nM 8.80
CHEMBL1945292 — EC50 = 1.995 nM 8.70
CHEMBL1945503 — EC50 = 2.512 nM 8.60
CHEMBL1945298 — EC50 = 2.512 nM 8.60
CHEMBL1945291 — EC50 = 3.162 nM 8.50
CHEMBL1945290 — EC50 = 3.162 nM 8.50
CHEMBL1945040 — EC50 = 3.162 nM 8.50
CHEMBL1947155 — EC50 = 3.981 nM 8.40
CHEMBL1946765 — EC50 = 3.981 nM 8.40
CHEMBL1945504 — EC50 = 7.943 nM 8.10
CHEMBL1947154 — EC50 = 10.0 nM 8.00
CHEMBL1945293 — EC50 = 15.85 nM 7.80
CHEMBL1095777 INDACATEROL EC50 = 15.85 nM 7.80
CHEMBL1945300 — EC50 = 31.62 nM 7.50
CHEMBL1945295 — EC50 = 39.81 nM 7.40
CHEMBL1946762 — EC50 = 79.43 nM 7.10
CHEMBL1946761 — EC50 = 100.0 nM 7.00
CHEMBL1946763 — EC50 = 158.49 nM 6.80
CHEMBL1946764 — EC50 = 158.49 nM 6.80
CHEMBL1946766 — EC50 = 316.23 nM 6.50