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Assay Detail

CHEMBL650012

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

Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL ↗
53
Total Activities
53
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Beta-1 adrenergic receptor (CHEMBL5471) ↗
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 53 7.96 9.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL499 TIMOLOL 4.0 1 9.44
CHEMBL11671 — — 1 9.07
CHEMBL3392321 — — 1 9.03
CHEMBL11171 — — 1 8.92
CHEMBL11145 — — 1 8.84
CHEMBL27 PROPRANOLOL 4.0 1 8.76
CHEMBL423 BETAXOLOL 4.0 1 8.76
CHEMBL11051 — — 1 8.71
CHEMBL416150 — — 1 8.69
CHEMBL11112 — — 1 8.54
CHEMBL11205 — — 1 8.54
CHEMBL415970 — — 1 8.51
CHEMBL11396 — — 1 8.46
CHEMBL11431 — — 1 8.30
CHEMBL11178 — — 1 8.29
CHEMBL11406 — — 1 8.22
CHEMBL2052005 — — 1 8.19
CHEMBL11080 — — 1 8.16
CHEMBL11092 — — 1 8.12
CHEMBL11224 — — 1 8.10
CHEMBL10988 — — 1 8.00
CHEMBL65774 — — 1 7.97
CHEMBL10998 — — 1 7.96
CHEMBL10813 — — 1 7.94
CHEMBL10574 — — 1 7.89
CHEMBL416151 — — 1 7.89
CHEMBL11093 — — 1 7.88
CHEMBL10983 — — 1 7.83
CHEMBL13 METOPROLOL 4.0 1 7.83
CHEMBL274830 — — 1 7.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL499 TIMOLOL Kd = 0.3631 nM 9.44
CHEMBL11671 — Kd = 0.8511 nM 9.07
CHEMBL3392321 — Kd = 0.9333 nM 9.03
CHEMBL11171 — Kd = 1.202 nM 8.92
CHEMBL11145 — Kd = 1.445 nM 8.84
CHEMBL27 PROPRANOLOL Kd = 1.738 nM 8.76
CHEMBL423 BETAXOLOL Kd = 1.738 nM 8.76
CHEMBL11051 — Kd = 1.95 nM 8.71
CHEMBL416150 — Kd = 2.042 nM 8.69
CHEMBL11112 — Kd = 2.884 nM 8.54
CHEMBL11205 — Kd = 2.884 nM 8.54
CHEMBL415970 — Kd = 3.09 nM 8.51
CHEMBL11396 — Kd = 3.467 nM 8.46
CHEMBL11431 — Kd = 5.012 nM 8.30
CHEMBL11178 — Kd = 5.129 nM 8.29
CHEMBL11406 — Kd = 6.026 nM 8.22
CHEMBL2052005 — Kd = 6.457 nM 8.19
CHEMBL11080 — Kd = 6.918 nM 8.16
CHEMBL11092 — Kd = 7.586 nM 8.12
CHEMBL11224 — Kd = 7.943 nM 8.10
CHEMBL10988 — Kd = 10.0 nM 8.00
CHEMBL65774 — Kd = 10.72 nM 7.97
CHEMBL10998 — Kd = 10.96 nM 7.96
CHEMBL10813 — Kd = 11.48 nM 7.94
CHEMBL416151 — Kd = 12.88 nM 7.89
CHEMBL10574 — Kd = 12.88 nM 7.89
CHEMBL11093 — Kd = 13.18 nM 7.88
CHEMBL10983 — Kd = 14.79 nM 7.83
CHEMBL13 METOPROLOL Kd = 14.79 nM 7.83
CHEMBL274830 — Kd = 15.85 nM 7.80
CHEMBL275934 — Kd = 16.6 nM 7.78
CHEMBL2052004 — Kd = 16.98 nM 7.77
CHEMBL63421 — Kd = 17.38 nM 7.76
CHEMBL442522 — Kd = 18.62 nM 7.73
CHEMBL11135 — Kd = 19.05 nM 7.72
CHEMBL2052006 — Kd = 19.95 nM 7.70
CHEMBL269467 — Kd = 21.88 nM 7.66
CHEMBL11097 — Kd = 22.39 nM 7.65
CHEMBL269219 — Kd = 23.44 nM 7.63
CHEMBL24 ATENOLOL Kd = 23.99 nM 7.62
CHEMBL11414 — Kd = 24.55 nM 7.61
CHEMBL1788320 — Kd = 29.51 nM 7.53
CHEMBL11427 — Kd = 30.9 nM 7.51
CHEMBL11467 — Kd = 43.65 nM 7.36
CHEMBL276029 — Kd = 43.65 nM 7.36
CHEMBL10879 — Kd = 50.12 nM 7.30
CHEMBL11155 — Kd = 58.88 nM 7.23
CHEMBL11362 — Kd = 61.66 nM 7.21
CHEMBL11219 — Kd = 93.33 nM 7.03
CHEMBL536552 — Kd = 478.63 nM 6.32