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Assay Detail

CHEMBL652054

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

Binding
Binding affinity to CHO cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Beta-3 adrenergic receptor (CHEMBL246)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

BMS-196085: a potent and selective full agonist of the human beta(3) adrenergic receptor.
Gavai AV, Sher PM, Mikkilineni AB, Poss KM, McCann PJ, Girotra RN, Fisher LG, Wu G, Bednarz MS, Mathur A, Wang TC, Sun CQ, Slusarchyk DA, Skwish S, Allen GT, Hillyer DE, Frohlich BH, Abboa-Offei BE, Cap M, Waldron TL, George RJ, Tesfamariam B, Harper TW, Ciosek CP, Young DA, Dickinson KE, Seymour AA, Arbeeny CM, Washburn WN.
Bioorg Med Chem Lett (2001) 11 : 3041 -3044
PubMed 11714606 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 30 6.96 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL105758 1 8.70
CHEMBL321518 1 8.10
CHEMBL317648 1 8.05
CHEMBL102611 1 7.82
CHEMBL322862 1 7.68
CHEMBL102580 1 7.60
CHEMBL317920 1 7.58
CHEMBL319687 1 7.42
CHEMBL431638 1 7.37
CHEMBL102928 1 7.36
CHEMBL274494 1 7.16
CHEMBL105475 1 7.16
CHEMBL104905 1 7.16
CHEMBL319186 1 7.13
CHEMBL104988 1 7.08
CHEMBL105004 1 7.07
CHEMBL102813 1 6.92
CHEMBL100138 1 6.89
CHEMBL104899 1 6.83
CHEMBL104217 1 6.68
CHEMBL103117 1 6.68
CHEMBL318074 1 6.64
CHEMBL102257 1 6.44
CHEMBL103118 1 6.36
CHEMBL105559 1 6.16
CHEMBL409312 1 6.10
CHEMBL102177 1 6.08
CHEMBL102701 1 6.00
CHEMBL320818 1 5.62
CHEMBL320667 1 5.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL105758 Ki = 2.0 nM 8.70
CHEMBL321518 Ki = 8.0 nM 8.10
CHEMBL317648 Ki = 9.0 nM 8.05
CHEMBL102611 Ki = 15.0 nM 7.82
CHEMBL322862 Ki = 21.0 nM 7.68
CHEMBL102580 Ki = 25.0 nM 7.60
CHEMBL317920 Ki = 26.0 nM 7.58
CHEMBL319687 Ki = 38.0 nM 7.42
CHEMBL431638 Ki = 43.0 nM 7.37
CHEMBL102928 Ki = 44.0 nM 7.36
CHEMBL274494 Ki = 70.0 nM 7.16
CHEMBL105475 Ki = 70.0 nM 7.16
CHEMBL104905 Ki = 69.0 nM 7.16
CHEMBL319186 Ki = 74.0 nM 7.13
CHEMBL104988 Ki = 84.0 nM 7.08
CHEMBL105004 Ki = 85.0 nM 7.07
CHEMBL102813 Ki = 120.0 nM 6.92
CHEMBL100138 Ki = 129.0 nM 6.89
CHEMBL104899 Ki = 147.0 nM 6.83
CHEMBL104217 Ki = 210.0 nM 6.68
CHEMBL103117 Ki = 210.0 nM 6.68
CHEMBL318074 Ki = 230.0 nM 6.64
CHEMBL102257 Ki = 360.0 nM 6.44
CHEMBL103118 Ki = 440.0 nM 6.36
CHEMBL105559 Ki = 700.0 nM 6.16
CHEMBL409312 Ki = 800.0 nM 6.10
CHEMBL102177 Ki = 836.0 nM 6.08
CHEMBL102701 Ki = 990.0 nM 6.00
CHEMBL320818 Ki = 2400.0 nM 5.62
CHEMBL320667 Ki = 8600.0 nM 5.07