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Assay Detail

CHEMBL888301

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

Binding
Displacement of [125I]iodocyanopindolol from cloned human adrenergic beta-3 receptor expressed in CHO cells
42
Total Activities
42
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-3 adrenergic receptor (CHEMBL246)
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 42 7.05 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL250978 1 8.52
CHEMBL401135 1 8.30
CHEMBL399329 1 8.22
CHEMBL250755 1 8.22
CHEMBL447786 1 8.15
CHEMBL437578 1 8.15
CHEMBL250191 1 8.15
CHEMBL400947 1 8.10
CHEMBL398557 1 8.05
CHEMBL400067 1 8.05
CHEMBL317621 1 7.96
CHEMBL251764 1 7.92
CHEMBL250553 1 7.72
CHEMBL322862 1 7.68
CHEMBL429665 1 7.62
CHEMBL248548 1 7.60
CHEMBL398241 1 7.54
CHEMBL251347 1 7.51
CHEMBL251581 1 7.28
CHEMBL251555 1 7.23
CHEMBL117577 1 7.11
CHEMBL102836 1 7.09
CHEMBL398322 1 6.96
CHEMBL249359 1 6.88
CHEMBL440961 1 6.82
CHEMBL251370 1 6.80
CHEMBL428584 1 6.77
CHEMBL438343 1 6.70
CHEMBL251361 1 6.57
CHEMBL399867 1 6.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL250978 Ki = 3.0 nM 8.52
CHEMBL401135 Ki = 5.0 nM 8.30
CHEMBL250755 Ki = 6.0 nM 8.22
CHEMBL399329 Ki = 6.0 nM 8.22
CHEMBL447786 Ki = 7.0 nM 8.15
CHEMBL437578 Ki = 7.0 nM 8.15
CHEMBL250191 Ki = 7.0 nM 8.15
CHEMBL400947 Ki = 8.0 nM 8.10
CHEMBL398557 Ki = 9.0 nM 8.05
CHEMBL400067 Ki = 9.0 nM 8.05
CHEMBL317621 Ki = 11.0 nM 7.96
CHEMBL251764 Ki = 12.0 nM 7.92
CHEMBL250553 Ki = 19.0 nM 7.72
CHEMBL322862 Ki = 21.0 nM 7.68
CHEMBL429665 Ki = 24.0 nM 7.62
CHEMBL248548 Ki = 25.0 nM 7.60
CHEMBL398241 Ki = 29.0 nM 7.54
CHEMBL251347 Ki = 31.0 nM 7.51
CHEMBL251581 Ki = 53.0 nM 7.28
CHEMBL251555 Ki = 59.0 nM 7.23
CHEMBL117577 Ki = 77.0 nM 7.11
CHEMBL102836 Ki = 81.0 nM 7.09
CHEMBL398322 Ki = 110.0 nM 6.96
CHEMBL249359 Ki = 133.0 nM 6.88
CHEMBL440961 Ki = 150.0 nM 6.82
CHEMBL251370 Ki = 160.0 nM 6.80
CHEMBL428584 Ki = 170.0 nM 6.77
CHEMBL438343 Ki = 200.0 nM 6.70
CHEMBL251361 Ki = 270.0 nM 6.57
CHEMBL399867 Ki = 340.0 nM 6.47
CHEMBL400669 Ki = 360.0 nM 6.44
CHEMBL251554 Ki = 390.0 nM 6.41
CHEMBL251580 Ki = 460.0 nM 6.34
CHEMBL401334 Ki = 880.0 nM 6.06
CHEMBL250954 Ki = 1100.0 nM 5.96
CHEMBL398320 Ki = 1100.0 nM 5.96
CHEMBL251362 Ki = 1700.0 nM 5.77
CHEMBL251175 Ki = 3700.0 nM 5.43
CHEMBL399866 Ki = 7300.0 nM 5.14
CHEMBL251363 Ki = 15000.0 nM 4.82
CHEMBL400645 Ki = 17000.0 nM 4.77
CHEMBL251166 Ki = 120000.0 nM -