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Assay Detail

CHEMBL748003

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

Binding
In vitro binding affinity towards Norepinephrine transporter rat cerebral cortical homogenates by [3H]nisoxetine displacement.
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Norepinephrine transporter (CHEMBL304)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

N-substituted analogs of 2 beta-carbomethoxy-3 beta- (4'-iodophenyl)tropane (beta-CIT) with selective affinity to dopamine or serotonin transporters in rat forebrain.
Neumeyer JL, Tamagnan G, Wang S, Gao Y, Milius RA, Kula NS, Baldessarini RJ.
J Med Chem (1996) 39 : 543 -548
PubMed 8558525 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 6.64 8.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL14391 1 8.55
CHEMBL149801 1 7.54
CHEMBL318755 1 7.20
CHEMBL2112550 1 7.13
CHEMBL358006 1 7.03
CHEMBL345553 1 7.02
CHEMBL153361 1 6.96
CHEMBL356652 1 6.79
CHEMBL150084 1 6.70
CHEMBL357300 1 6.66
CHEMBL2112890 1 6.28
CHEMBL2079586 1 6.20
CHEMBL153602 1 5.30
CHEMBL153200 1 5.30
CHEMBL345760 1 5.00
CHEMBL356166 1 -
CHEMBL281594 VANOXERINE 3.0 1 -
CHEMBL370805 COCAINE 4.0 1 -
CHEMBL346872 1 -
CHEMBL153121 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL14391 Ki = 2.8 nM 8.55
CHEMBL149801 Ki = 29.1 nM 7.54
CHEMBL318755 Ki = 63.0 nM 7.20
CHEMBL2112550 Ki = 73.7 nM 7.13
CHEMBL358006 Ki = 93.0 nM 7.03
CHEMBL345553 Ki = 96.0 nM 7.02
CHEMBL153361 Ki = 110.0 nM 6.96
CHEMBL356652 Ki = 164.0 nM 6.79
CHEMBL150084 Ki = 198.0 nM 6.70
CHEMBL357300 Ki = 217.0 nM 6.66
CHEMBL2112890 Ki = 522.0 nM 6.28
CHEMBL2079586 Ki = 635.0 nM 6.20
CHEMBL153602 Ki = 5000.0 nM 5.30
CHEMBL153200 Ki = 5000.0 nM 5.30
CHEMBL345760 Ki = 10000.0 nM 5.00
CHEMBL356166 Ki > 5000.0 nM -
CHEMBL281594 VANOXERINE Ki > 20000.0 nM -
CHEMBL370805 COCAINE Ki > 30000.0 nM -
CHEMBL346872 Ki > 10000.0 nM -
CHEMBL153121 Ki > 10000.0 nM -