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Assay Detail

CHEMBL652052

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

Binding
Binding affinity towards human beta-3 adrenergic receptor expressed in CHO cells
48
Total Activities
46
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-201620: a selective beta 3 agonist.
Washburn WN, Sun CQ, Bisacchi G, Wu G, Cheng PT, Sher PM, Ryono D, Gavai AV, Poss K, Girotra RN, McCann PJ, Mikkilineni AB, Dejneka TC, Wang TC, Merchant Z, Morella M, Arbeeny CM, Harper TW, Slusarchyk DA, Skwish S, Russell AD, Allen GT, Tesfamariam B, Frohlich BH, Abboa-Offei BE, Cap M, Waldron TL, George RJ, Young D, Dickinson KE, Seymour AA.
Bioorg Med Chem Lett (2004) 14 : 3525 -3529
PubMed 15177466 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 48 6.59 8.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL323938 1 8.06
CHEMBL332529 1 7.96
CHEMBL119120 1 7.85
CHEMBL115628 1 7.77
CHEMBL434223 1 7.77
CHEMBL119533 1 7.72
CHEMBL326820 1 7.70
CHEMBL116294 1 7.64
CHEMBL118121 1 7.62
CHEMBL119786 1 7.55
CHEMBL333334 2 7.48
CHEMBL116715 1 7.36
CHEMBL332632 1 7.34
CHEMBL115627 1 7.33
CHEMBL333551 1 7.29
CHEMBL115538 1 7.21
CHEMBL117737 1 7.15
CHEMBL117577 2 7.11
CHEMBL102836 1 7.09
CHEMBL118216 1 7.05
CHEMBL325425 1 7.03
CHEMBL119070 1 6.94
CHEMBL118675 1 6.85
CHEMBL116080 1 6.72
CHEMBL418867 1 6.58
CHEMBL119860 1 6.47
CHEMBL118834 1 6.43
CHEMBL330924 1 6.43
CHEMBL115424 1 6.42
CHEMBL115972 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL323938 Ki = 8.8 nM 8.06
CHEMBL332529 Ki = 11.0 nM 7.96
CHEMBL119120 Ki = 14.0 nM 7.85
CHEMBL115628 Ki = 17.0 nM 7.77
CHEMBL434223 Ki = 17.0 nM 7.77
CHEMBL119533 Ki = 19.0 nM 7.72
CHEMBL326820 Ki = 20.0 nM 7.70
CHEMBL116294 Ki = 23.0 nM 7.64
CHEMBL118121 Ki = 24.0 nM 7.62
CHEMBL119786 Ki = 28.0 nM 7.55
CHEMBL333334 Ki = 33.0 nM 7.48
CHEMBL116715 Ki = 44.0 nM 7.36
CHEMBL332632 Ki = 46.0 nM 7.34
CHEMBL115627 Ki = 47.0 nM 7.33
CHEMBL333551 Ki = 51.0 nM 7.29
CHEMBL115538 Ki = 61.0 nM 7.21
CHEMBL117737 Ki = 71.0 nM 7.15
CHEMBL117577 Ki = 77.0 nM 7.11
CHEMBL102836 Ki = 81.0 nM 7.09
CHEMBL118216 Ki = 89.0 nM 7.05
CHEMBL325425 Ki = 93.0 nM 7.03
CHEMBL119070 Ki = 115.0 nM 6.94
CHEMBL118675 Ki = 142.0 nM 6.85
CHEMBL116080 Ki = 190.0 nM 6.72
CHEMBL418867 Ki = 260.0 nM 6.58
CHEMBL333334 Ki = 280.0 nM 6.55
CHEMBL119860 Ki = 340.0 nM 6.47
CHEMBL117577 Ki = 370.0 nM 6.43
CHEMBL118834 Ki = 370.0 nM 6.43
CHEMBL330924 Ki = 370.0 nM 6.43
CHEMBL115424 Ki = 380.0 nM 6.42
CHEMBL115972 Ki = 400.0 nM 6.40
CHEMBL326612 Ki = 450.0 nM 6.35
CHEMBL117596 Ki = 490.0 nM 6.31
CHEMBL331027 Ki = 520.0 nM 6.28
CHEMBL119875 Ki = 950.0 nM 6.02
CHEMBL261933 Ki = 1800.0 nM 5.75
CHEMBL119128 Ki = 2200.0 nM 5.66
CHEMBL118287 Ki = 2910.0 nM 5.54
CHEMBL119831 Ki = 3100.0 nM 5.51
CHEMBL325853 Ki = 3100.0 nM 5.51
CHEMBL118336 Ki = 7000.0 nM 5.16
CHEMBL118069 Ki = 8200.0 nM 5.09
CHEMBL333879 Ki = 9600.0 nM 5.02
CHEMBL119210 Ki = 10000.0 nM 5.00
CHEMBL2111776 Ki = 14100.0 nM 4.85
CHEMBL2111775 Ki = 30000.0 nM 4.52
CHEMBL119539 Ki = 33000.0 nM 4.48