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Assay Detail

CHEMBL651636

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

Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL ↗
50
Total Activities
50
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Beta-2 adrenergic receptor (CHEMBL5414) ↗
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Beta 1-selective adrenoceptor antagonists: examples of the 2-[4-[3-(substituted amino)-2-hydroxypropoxy]phenyl]imidazole class. 2.
Baldwin JJ, Christy ME, Denny GH, Habecker CN, Freedman MB, Lyle PA, Ponticello GS, Varga SL, Gross DM, Sweet CS.
J Med Chem (1986) 29 : 1065 -1080
PubMed 2872332 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 49 5.44 9.01
pA2 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27 PROPRANOLOL 4.0 1 9.01
CHEMBL11125 — — 1 7.61
CHEMBL1788320 — — 1 7.19
CHEMBL423 BETAXOLOL 4.0 1 6.98
CHEMBL13 METOPROLOL 4.0 1 6.79
CHEMBL11135 — — 1 6.70
CHEMBL11362 — — 1 6.68
CHEMBL11171 — — 1 6.61
CHEMBL3392321 — — 1 6.08
CHEMBL416150 — — 1 6.04
CHEMBL2052005 — — 1 5.97
CHEMBL24 ATENOLOL 4.0 1 5.93
CHEMBL11092 — — 1 5.81
CHEMBL10988 — — 1 5.81
CHEMBL11080 — — 1 5.68
CHEMBL11051 — — 1 5.66
CHEMBL269467 — — 1 5.50
CHEMBL11406 — — 1 5.46
CHEMBL275934 — — 1 5.46
CHEMBL11396 — — 1 5.42
CHEMBL415970 — — 1 5.40
CHEMBL442522 — — 1 5.36
CHEMBL11307 — — 1 5.28
CHEMBL269219 — — 1 5.26
CHEMBL10574 — — 1 5.25
CHEMBL11224 — — 1 5.23
CHEMBL274830 — — 1 5.19
CHEMBL11671 — — 1 5.13
CHEMBL11178 — — 1 5.07
CHEMBL11097 — — 1 4.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27 PROPRANOLOL Kd = 0.9772 nM 9.01
CHEMBL11125 — Kd = 24.55 nM 7.61
CHEMBL1788320 — Kd = 64.57 nM 7.19
CHEMBL423 BETAXOLOL Kd = 104.71 nM 6.98
CHEMBL13 METOPROLOL Kd = 162.18 nM 6.79
CHEMBL11135 — Kd = 199.53 nM 6.70
CHEMBL11362 — Kd = 208.93 nM 6.68
CHEMBL11171 — Kd = 245.47 nM 6.61
CHEMBL3392321 — Kd = 831.76 nM 6.08
CHEMBL416150 — Kd = 912.01 nM 6.04
CHEMBL2052005 — Kd = 1071.52 nM 5.97
CHEMBL24 ATENOLOL Kd = 1174.9 nM 5.93
CHEMBL11092 — Kd = 1548.82 nM 5.81
CHEMBL10988 — Kd = 1548.82 nM 5.81
CHEMBL11080 — Kd = 2089.3 nM 5.68
CHEMBL11051 — Kd = 2187.76 nM 5.66
CHEMBL269467 — Kd = 3162.28 nM 5.50
CHEMBL11406 — Kd = 3467.37 nM 5.46
CHEMBL275934 — Kd = 3467.37 nM 5.46
CHEMBL11396 — Kd = 3801.89 nM 5.42
CHEMBL415970 — Kd = 3981.07 nM 5.40
CHEMBL442522 — Kd = 4365.16 nM 5.36
CHEMBL11307 — Kd = 5248.07 nM 5.28
CHEMBL269219 — Kd = 5495.41 nM 5.26
CHEMBL10574 — Kd = 5623.41 nM 5.25
CHEMBL11224 — Kd = 5888.44 nM 5.23
CHEMBL274830 — Kd = 6456.54 nM 5.19
CHEMBL11671 — Kd = 7413.1 nM 5.13
CHEMBL11178 — Kd = 8511.38 nM 5.07
CHEMBL11097 — Kd = 10715.19 nM 4.97
CHEMBL10825 — Kd = 16595.87 nM 4.78
CHEMBL10983 — Kd = 17378.01 nM 4.76
CHEMBL11093 — Kd = 17782.79 nM 4.75
CHEMBL11431 — Kd = 19952.62 nM 4.70
CHEMBL11401 — Kd = 21379.62 nM 4.67
CHEMBL2052006 — Kd = 25703.96 nM 4.59
CHEMBL10879 — Kd = 28840.32 nM 4.54
CHEMBL10813 — Kd = 31622.78 nM 4.50
CHEMBL416151 — Kd = 33884.42 nM 4.47
CHEMBL2052004 — Kd = 38018.94 nM 4.42
CHEMBL11427 — Kd = 40738.03 nM 4.39
CHEMBL11414 — Kd = 52480.75 nM 4.28
CHEMBL536552 — Kd = 53703.18 nM 4.27
CHEMBL276029 — Kd = 61659.5 nM 4.21
CHEMBL63421 — Kd = 63095.73 nM 4.20
CHEMBL11467 — Kd = 74131.02 nM 4.13
CHEMBL65774 — Kd > 100000.0 nM -
CHEMBL11205 — pA2 = - — -
CHEMBL11219 — Kd = 251188.64 nM -
CHEMBL11155 — Kd = 831763.77 nM -