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Assay Detail

CHEMBL888309

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

Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Arylpropanolamines: selective beta3 agonists arising from strategies to mitigate phase I metabolic transformations.
Washburn WN, Harper TW, Wu G, Godfrey JD, McCann P, Girotra R, Shao C, Zhang H, Gavai A, Mikkilineni A, Dejneka T, Ahmed S, Caringal Y, Hangeland J, Zhang M, Cheng PT, Russell AD, Skwish S, Slusarchyk DA, Allen GT, Frohlich BH, Abboa-Offei BE, Cap M, Waldron TL, George RJ, Tesfamariam B, Dickinson KE, Seymour AA, Sher PM.
Bioorg Med Chem Lett (2007) 17 : 4290 -4296
PubMed 17533126 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 6.64 7.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL398557 1 7.62
CHEMBL398241 1 7.58
CHEMBL249359 1 7.42
CHEMBL447786 1 7.24
CHEMBL399329 1 7.18
CHEMBL251555 1 7.15
CHEMBL250553 1 6.99
CHEMBL251764 1 6.92
CHEMBL251554 1 6.70
CHEMBL251347 1 6.55
CHEMBL398322 1 6.46
CHEMBL400067 1 6.41
CHEMBL251581 1 6.29
CHEMBL440961 1 6.09
CHEMBL400947 1 5.97
CHEMBL248548 1 5.82
CHEMBL398320 1 5.57
CHEMBL251580 1 5.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL398557 Ki = 24.0 nM 7.62
CHEMBL398241 Ki = 26.0 nM 7.58
CHEMBL249359 Ki = 38.0 nM 7.42
CHEMBL447786 Ki = 57.0 nM 7.24
CHEMBL399329 Ki = 66.0 nM 7.18
CHEMBL251555 Ki = 71.0 nM 7.15
CHEMBL250553 Ki = 102.0 nM 6.99
CHEMBL251764 Ki = 120.0 nM 6.92
CHEMBL251554 Ki = 200.0 nM 6.70
CHEMBL251347 Ki = 280.0 nM 6.55
CHEMBL398322 Ki = 350.0 nM 6.46
CHEMBL400067 Ki = 390.0 nM 6.41
CHEMBL251581 Ki = 510.0 nM 6.29
CHEMBL440961 Ki = 820.0 nM 6.09
CHEMBL400947 Ki = 1070.0 nM 5.97
CHEMBL248548 Ki = 1500.0 nM 5.82
CHEMBL398320 Ki = 2700.0 nM 5.57
CHEMBL251580 Ki = 3100.0 nM 5.51