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Assay Detail

CHEMBL641156

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

Binding
In vitro binding affinity against alpha-2 adrenergic receptor of rat in presence of [3H]-RX 821002 radioligand
ChEMBL ↗
52
Total Activities
52
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

Potential antidepressants displayed combined alpha(2)-adrenoceptor antagonist and monoamine uptake inhibitor properties.
Cordi AA, Berque-Bestel I, Persigand T, Lacoste JM, Newman-Tancredi A, Audinot V, Millan MJ.
J Med Chem (2001) 44 : 787 -805
PubMed 11262089 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 52 7.16 9.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL353972 ATIPAMEZOLE 2.0 1 9.90
CHEMBL167578 — — 1 9.10
CHEMBL355467 — — 1 8.90
CHEMBL168201 — — 1 8.90
CHEMBL166690 — — 1 8.80
CHEMBL353843 — — 1 8.70
CHEMBL167493 NAPAMEZOLE 2.0 1 8.50
CHEMBL354611 — — 1 8.20
CHEMBL90997 — — 1 8.10
CHEMBL165529 — — 1 8.00
CHEMBL167644 — — 1 7.90
CHEMBL166748 — — 1 7.80
CHEMBL166448 — — 1 7.80
CHEMBL353200 — — 1 7.60
CHEMBL168022 — — 1 7.60
CHEMBL352636 — — 1 7.60
CHEMBL168168 — — 1 7.50
CHEMBL167649 — — 1 7.50
CHEMBL353139 — — 1 7.40
CHEMBL166852 — — 1 7.30
CHEMBL352643 — — 1 7.30
CHEMBL166501 — — 1 7.30
CHEMBL353212 — — 1 7.30
CHEMBL168205 — — 1 7.20
CHEMBL166683 — — 1 7.10
CHEMBL166648 — — 1 7.10
CHEMBL407509 — — 1 7.00
CHEMBL165645 — — 1 7.00
CHEMBL168000 — — 1 6.90
CHEMBL262777 VANCOMYCIN 4.0 1 6.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL353972 ATIPAMEZOLE Ki = 0.1259 nM 9.90
CHEMBL167578 — Ki = 0.7943 nM 9.10
CHEMBL168201 — Ki = 1.259 nM 8.90
CHEMBL355467 — Ki = 1.259 nM 8.90
CHEMBL166690 — Ki = 1.585 nM 8.80
CHEMBL353843 — Ki = 1.995 nM 8.70
CHEMBL167493 NAPAMEZOLE Ki = 3.162 nM 8.50
CHEMBL354611 — Ki = 6.31 nM 8.20
CHEMBL90997 — Ki = 7.943 nM 8.10
CHEMBL165529 — Ki = 10.0 nM 8.00
CHEMBL167644 — Ki = 12.59 nM 7.90
CHEMBL166748 — Ki = 15.85 nM 7.80
CHEMBL166448 — Ki = 15.85 nM 7.80
CHEMBL352636 — Ki = 25.12 nM 7.60
CHEMBL353200 — Ki = 25.12 nM 7.60
CHEMBL168022 — Ki = 25.12 nM 7.60
CHEMBL168168 — Ki = 31.62 nM 7.50
CHEMBL167649 — Ki = 31.62 nM 7.50
CHEMBL353139 — Ki = 39.81 nM 7.40
CHEMBL166852 — Ki = 50.12 nM 7.30
CHEMBL352643 — Ki = 50.12 nM 7.30
CHEMBL166501 — Ki = 50.12 nM 7.30
CHEMBL353212 — Ki = 50.12 nM 7.30
CHEMBL168205 — Ki = 63.1 nM 7.20
CHEMBL166648 — Ki = 79.43 nM 7.10
CHEMBL166683 — Ki = 79.43 nM 7.10
CHEMBL407509 — Ki = 100.0 nM 7.00
CHEMBL165645 — Ki = 100.0 nM 7.00
CHEMBL168000 — Ki = 125.89 nM 6.90
CHEMBL262777 VANCOMYCIN Ki = 125.89 nM 6.90
CHEMBL164118 — Ki = 158.49 nM 6.80
CHEMBL354072 — Ki = 158.49 nM 6.80
CHEMBL436234 — Ki = 199.53 nM 6.70
CHEMBL354112 — Ki = 251.19 nM 6.60
CHEMBL165467 — Ki = 251.19 nM 6.60
CHEMBL168153 — Ki = 316.23 nM 6.50
CHEMBL167394 — Ki = 398.11 nM 6.40
CHEMBL3037826 — Ki = 398.11 nM 6.40
CHEMBL352704 — Ki = 398.11 nM 6.40
CHEMBL167665 — Ki = 501.19 nM 6.30
CHEMBL164070 — Ki = 501.19 nM 6.30
CHEMBL167749 — Ki = 630.96 nM 6.20
CHEMBL167795 — Ki = 630.96 nM 6.20
CHEMBL167437 — Ki = 794.33 nM 6.10
CHEMBL353910 — Ki = 794.33 nM 6.10
CHEMBL167515 — Ki = 1000.0 nM 6.00
CHEMBL353828 — Ki = 1000.0 nM 6.00
CHEMBL424557 — Ki = 1584.89 nM 5.80
CHEMBL168063 — Ki = 1584.89 nM 5.80
CHEMBL166226 — Ki = 3162.28 nM 5.50