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Assay Detail

CHEMBL2434576

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

Binding
Binding affinity at human alpha2B AR
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Alpha-2B adrenergic receptor (CHEMBL1942)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity.
Del Bello F, Diamanti E, Giannella M, Mammoli V, Mattioli L, Titomanlio F, Piergentili A, Quaglia W, Lanza M, Sabatini C, Caselli G, Poggesi E, Pigini M.
ACS Med Chem Lett (2013) 4 : 875 -879
PubMed 24900763 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 6.23 6.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1276220 1 6.58
CHEMBL1276218 1 6.51
CHEMBL2089155 1 6.47
CHEMBL495095 ALLYPHENYLINE 1 6.47
CHEMBL1956192 1 6.45
CHEMBL1276140 1 6.40
CHEMBL1956195 CYCLOMETHYLINE 1 6.39
CHEMBL2089156 1 6.39
CHEMBL2431281 1 6.30
CHEMBL13852 CIRAZOLINE 2.0 1 6.28
CHEMBL2431282 1 6.27
CHEMBL13917 1 6.26
CHEMBL1276139 1 6.25
CHEMBL1276219 1 6.25
CHEMBL2431279 1 6.21
CHEMBL14107 1 6.15
CHEMBL2431280 1 6.10
CHEMBL1956197 1 5.98
CHEMBL404505 1 4.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1276220 Ki = 263.03 nM 6.58
CHEMBL1276218 Ki = 309.03 nM 6.51
CHEMBL2089155 Ki = 338.84 nM 6.47
CHEMBL495095 ALLYPHENYLINE Ki = 338.84 nM 6.47
CHEMBL1956192 Ki = 354.81 nM 6.45
CHEMBL1276140 Ki = 398.11 nM 6.40
CHEMBL1956195 CYCLOMETHYLINE Ki = 407.38 nM 6.39
CHEMBL2089156 Ki = 407.38 nM 6.39
CHEMBL2431281 Ki = 501.19 nM 6.30
CHEMBL13852 CIRAZOLINE Ki = 524.81 nM 6.28
CHEMBL2431282 Ki = 537.03 nM 6.27
CHEMBL13917 Ki = 549.54 nM 6.26
CHEMBL1276139 Ki = 562.34 nM 6.25
CHEMBL1276219 Ki = 562.34 nM 6.25
CHEMBL2431279 Ki = 616.6 nM 6.21
CHEMBL14107 Ki = 707.95 nM 6.15
CHEMBL2431280 Ki = 794.33 nM 6.10
CHEMBL1956197 Ki = 1047.13 nM 5.98
CHEMBL404505 Ki = 26915.35 nM 4.57