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Assay Detail

CHEMBL648713

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

Binding
Binding affinity at alpha-2 adrenergic receptors of rat.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-2 (CHEMBL2093864)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Binding of beta-carbolines at imidazoline I2 receptors: a structure-affinity investigation.
Glennon RA, Grella B, Tyacke RJ, Lau A, Westaway J, Hudson AL.
Bioorg Med Chem Lett (2004) 14 : 999 -1002
PubMed 15013009 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 5.60 6.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6591 1 6.48
CHEMBL6426 1 6.41
CHEMBL6557 PNU-22394 1 6.38
CHEMBL269074 1 6.22
CHEMBL269571 1 6.19
CHEMBL266221 1 6.16
CHEMBL6746 1 6.09
CHEMBL6586 1 6.08
CHEMBL269236 TRYPTOLINE 1 5.80
CHEMBL6717 1 5.66
CHEMBL267599 1 5.50
CHEMBL269367 1 5.30
CHEMBL6626 1 5.28
CHEMBL266084 1 5.11
CHEMBL6310 1 5.05
CHEMBL428999 1 4.97
CHEMBL6427 1 4.94
CHEMBL6509 1 4.83
CHEMBL441891 1 4.81
CHEMBL6640 TRYPTAMINE 1 4.72
CHEMBL6409 CGS-19281A 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6591 Ki = 330.0 nM 6.48
CHEMBL6426 Ki = 390.0 nM 6.41
CHEMBL6557 PNU-22394 Ki = 415.0 nM 6.38
CHEMBL269074 Ki = 600.0 nM 6.22
CHEMBL269571 Ki = 640.0 nM 6.19
CHEMBL266221 Ki = 700.0 nM 6.16
CHEMBL6746 Ki = 815.0 nM 6.09
CHEMBL6586 Ki = 825.0 nM 6.08
CHEMBL269236 TRYPTOLINE Ki = 1600.0 nM 5.80
CHEMBL6717 Ki = 2190.0 nM 5.66
CHEMBL267599 Ki = 3160.0 nM 5.50
CHEMBL269367 Ki = 5020.0 nM 5.30
CHEMBL6626 Ki = 5290.0 nM 5.28
CHEMBL266084 Ki = 7830.0 nM 5.11
CHEMBL6310 Ki = 8840.0 nM 5.05
CHEMBL428999 Ki = 10700.0 nM 4.97
CHEMBL6427 Ki = 11500.0 nM 4.94
CHEMBL6509 Ki = 14700.0 nM 4.83
CHEMBL441891 Ki = 15500.0 nM 4.81
CHEMBL6640 TRYPTAMINE Ki = 19000.0 nM 4.72
CHEMBL6409 CGS-19281A Ki > 10000.0 nM -