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Assay Detail

CHEMBL652585

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

Binding
Binding affinity against CHO cells transfected with human beta-3 adrenergic receptor in the presence of [125I]iodocyanopindolol
38
Total Activities
38
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

Beta 3 agonists. Part 1: evolution from inception to BMS-194449.
Washburn WN, Sher PM, Poss KM, Girotra RN, McCann PJ, Gavai AV, Mikkilineni AB, Mathur A, Cheng P, Dejneka TC, Sun CQ, Wang TC, Harper TW, Russell AD, Slusarchyk DA, Skwish S, Allen GT, Hillyer DE, Frohlich BH, Abboa-Offei BE, Cap M, Waldron TL, George RJ, Tesfamariam B, Ciosek CP, Ryono D, Young DA, Dickinson KE, Seymour AA, Arbeeny CM, Gregg RE.
Bioorg Med Chem Lett (2001) 11 : 3035 -3039
PubMed 11714605 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 38 6.15 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL317621 1 7.96
CHEMBL102222 1 7.70
CHEMBL102891 1 7.48
CHEMBL102928 1 7.36
CHEMBL103147 1 7.16
CHEMBL102836 1 7.09
CHEMBL103131 1 7.09
CHEMBL319257 1 6.88
CHEMBL320915 1 6.80
CHEMBL102759 1 6.66
CHEMBL103784 1 6.64
CHEMBL322863 1 6.52
CHEMBL101591 1 6.50
CHEMBL106329 1 6.50
CHEMBL102257 1 6.44
CHEMBL321987 1 6.38
CHEMBL102522 1 6.32
CHEMBL103219 1 6.32
CHEMBL405622 1 6.28
CHEMBL316546 1 6.26
CHEMBL102364 1 6.24
CHEMBL284782 1 6.18
CHEMBL323091 1 6.01
CHEMBL105392 1 5.96
CHEMBL103743 1 5.82
CHEMBL318579 1 5.81
CHEMBL105095 1 5.80
CHEMBL102471 1 5.55
CHEMBL105430 1 5.48
CHEMBL102291 1 5.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL317621 Ki = 11.0 nM 7.96
CHEMBL102222 Ki = 20.0 nM 7.70
CHEMBL102891 Ki = 33.0 nM 7.48
CHEMBL102928 Ki = 44.0 nM 7.36
CHEMBL103147 Ki = 70.0 nM 7.16
CHEMBL102836 Ki = 81.0 nM 7.09
CHEMBL103131 Ki = 81.0 nM 7.09
CHEMBL319257 Ki = 133.0 nM 6.88
CHEMBL320915 Ki = 160.0 nM 6.80
CHEMBL102759 Ki = 220.0 nM 6.66
CHEMBL103784 Ki = 230.0 nM 6.64
CHEMBL322863 Ki = 300.0 nM 6.52
CHEMBL101591 Ki = 320.0 nM 6.50
CHEMBL106329 Ki = 320.0 nM 6.50
CHEMBL102257 Ki = 360.0 nM 6.44
CHEMBL321987 Ki = 414.0 nM 6.38
CHEMBL102522 Ki = 480.0 nM 6.32
CHEMBL103219 Ki = 480.0 nM 6.32
CHEMBL405622 Ki = 520.0 nM 6.28
CHEMBL316546 Ki = 550.0 nM 6.26
CHEMBL102364 Ki = 570.0 nM 6.24
CHEMBL284782 Ki = 660.0 nM 6.18
CHEMBL323091 Ki = 980.0 nM 6.01
CHEMBL105392 Ki = 1100.0 nM 5.96
CHEMBL103743 Ki = 1500.0 nM 5.82
CHEMBL318579 Ki = 1550.0 nM 5.81
CHEMBL105095 Ki = 1600.0 nM 5.80
CHEMBL102471 Ki = 2800.0 nM 5.55
CHEMBL105430 Ki = 3300.0 nM 5.48
CHEMBL102291 Ki = 3700.0 nM 5.43
CHEMBL30746 SOTERENOL Ki = 4100.0 nM 5.39
CHEMBL317852 Ki = 4300.0 nM 5.37
CHEMBL105603 Ki = 5800.0 nM 5.24
CHEMBL101693 Ki = 11000.0 nM 4.96
CHEMBL105019 Ki = 12700.0 nM 4.90
CHEMBL319632 Ki = 17000.0 nM 4.77
CHEMBL103096 Ki = 49000.0 nM 4.31
CHEMBL318830 Ki = 87000.0 nM 4.06