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Assay Detail

CHEMBL655218

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

Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Ultra-short-acting beta-adrenergic receptor blocking agents. 1. (Aryloxy)propanolamines containing esters in the nitrogen substituent.
Erhardt PW, Woo CM, Gorczynski RJ, Anderson WG.
J Med Chem (1982) 25 : 1402 -1407
PubMed 6130153 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 26 6.63 8.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL287651 1 8.90
CHEMBL31021 1 8.20
CHEMBL31529 1 8.10
CHEMBL31811 1 7.40
CHEMBL283289 1 7.40
CHEMBL32902 1 7.40
CHEMBL287242 1 7.30
CHEMBL31938 1 7.00
CHEMBL448775 1 7.00
CHEMBL31857 1 6.70
CHEMBL416030 1 6.70
CHEMBL32736 1 6.70
CHEMBL30942 1 6.60
CHEMBL31568 1 6.50
CHEMBL31888 1 6.30
CHEMBL31099 1 6.20
CHEMBL31611 1 6.20
CHEMBL282537 1 6.20
CHEMBL31050 1 6.00
CHEMBL284808 1 6.00
CHEMBL31772 1 5.90
CHEMBL281109 1 5.90
CHEMBL31598 1 5.70
CHEMBL31392 1 5.60
CHEMBL31411 1 5.60
CHEMBL288546 1 4.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL287651 Kd = 1.259 nM 8.90
CHEMBL31021 Kd = 6.31 nM 8.20
CHEMBL31529 Kd = 7.943 nM 8.10
CHEMBL31811 Kd = 39.81 nM 7.40
CHEMBL283289 Kd = 39.81 nM 7.40
CHEMBL32902 Kd = 39.81 nM 7.40
CHEMBL287242 Kd = 50.12 nM 7.30
CHEMBL31938 Kd = 100.0 nM 7.00
CHEMBL448775 Kd = 100.0 nM 7.00
CHEMBL31857 Kd = 199.53 nM 6.70
CHEMBL416030 Kd = 199.53 nM 6.70
CHEMBL32736 Kd = 199.53 nM 6.70
CHEMBL30942 Kd = 251.19 nM 6.60
CHEMBL31568 Kd = 316.23 nM 6.50
CHEMBL31888 Kd = 501.19 nM 6.30
CHEMBL31099 Kd = 630.96 nM 6.20
CHEMBL31611 Kd = 630.96 nM 6.20
CHEMBL282537 Kd = 630.96 nM 6.20
CHEMBL31050 Kd = 1000.0 nM 6.00
CHEMBL284808 Kd = 1000.0 nM 6.00
CHEMBL31772 Kd = 1258.93 nM 5.90
CHEMBL281109 Kd = 1258.93 nM 5.90
CHEMBL31598 Kd = 1995.26 nM 5.70
CHEMBL31392 Kd = 2511.89 nM 5.60
CHEMBL31411 Kd = 2511.89 nM 5.60
CHEMBL288546 Kd = 12589.25 nM 4.90