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Assay Detail

CHEMBL643713

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

Binding
In vitro binding affinity against alpha-2 adrenergic receptor in rat
35
Total Activities
35
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

Alpha(2) adrenoceptor agonists as potential analgesic agents. 1. (Imidazolylmethyl)oxazoles and -thiazoles.
Boyd RE, Press JB, Rasmussen CR, Raffa RB, Codd EE, Connelly CD, Bennett DJ, Kirifides AL, Gardocki JF, Reynolds B, Hortenstein JT, Reitz AB.
J Med Chem (1999) 42 : 5064 -5071
PubMed 10602691 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 35 7.37 10.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL778 DEXMEDETOMIDINE 4.0 1 10.82
CHEMBL358751 1 8.10
CHEMBL145852 1 8.00
CHEMBL358415 1 7.96
CHEMBL359068 1 7.89
CHEMBL358869 1 7.77
CHEMBL148566 1 7.75
CHEMBL150114 1 7.75
CHEMBL144495 1 7.75
CHEMBL145857 1 7.64
CHEMBL149704 1 7.55
CHEMBL342299 1 7.55
CHEMBL344743 1 7.46
CHEMBL148581 1 7.44
CHEMBL358978 1 7.43
CHEMBL149376 1 7.42
CHEMBL148857 ENTRY 68 A 1 7.28
CHEMBL146085 1 7.24
CHEMBL147194 1 7.24
CHEMBL423942 1 7.22
CHEMBL148701 1 7.07
CHEMBL348008 1 7.01
CHEMBL147774 1 7.01
CHEMBL150185 1 6.96
CHEMBL149672 1 6.63
CHEMBL148885 1 6.57
CHEMBL443289 1 6.54
CHEMBL346162 1 6.50
CHEMBL150064 1 6.42
CHEMBL145914 1 6.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL778 DEXMEDETOMIDINE Ki = 0.015 nM 10.82
CHEMBL358751 Ki = 8.0 nM 8.10
CHEMBL145852 Ki = 10.0 nM 8.00
CHEMBL358415 Ki = 11.0 nM 7.96
CHEMBL359068 Ki = 13.0 nM 7.89
CHEMBL358869 Ki = 17.0 nM 7.77
CHEMBL148566 Ki = 18.0 nM 7.75
CHEMBL150114 Ki = 18.0 nM 7.75
CHEMBL144495 Ki = 18.0 nM 7.75
CHEMBL145857 Ki = 23.0 nM 7.64
CHEMBL149704 Ki = 28.0 nM 7.55
CHEMBL342299 Ki = 28.0 nM 7.55
CHEMBL344743 Ki = 35.0 nM 7.46
CHEMBL148581 Ki = 36.0 nM 7.44
CHEMBL358978 Ki = 37.0 nM 7.43
CHEMBL149376 Ki = 38.0 nM 7.42
CHEMBL148857 ENTRY 68 A Ki = 53.0 nM 7.28
CHEMBL146085 Ki = 57.0 nM 7.24
CHEMBL147194 Ki = 58.0 nM 7.24
CHEMBL423942 Ki = 60.0 nM 7.22
CHEMBL148701 Ki = 86.0 nM 7.07
CHEMBL348008 Ki = 97.0 nM 7.01
CHEMBL147774 Ki = 97.0 nM 7.01
CHEMBL150185 Ki = 110.0 nM 6.96
CHEMBL149672 Ki = 235.0 nM 6.63
CHEMBL148885 Ki = 269.0 nM 6.57
CHEMBL443289 Ki = 285.0 nM 6.54
CHEMBL346162 Ki = 320.0 nM 6.50
CHEMBL150064 Ki = 381.0 nM 6.42
CHEMBL145914 Ki = 407.0 nM 6.39
CHEMBL145972 Ki = 714.0 nM 6.15
CHEMBL148827 Ki > 1000.0 nM -
CHEMBL147670 Ki > 1000.0 nM -
CHEMBL148160 Ki > 1000.0 nM -
CHEMBL148161 Ki > 1000.0 nM -