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Assay Detail

CHEMBL805319

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

Binding
Affinity at rat serotonin transporter using [125I]RTI-55 displacement.
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sodium-dependent serotonin transporter (CHEMBL313)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Structure-activity relationship studies of highly selective inhibitors of the dopamine transporter: N-benzylpiperidine analogues of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine.
Greiner E, Prisinzano T, Johnson EM, Dersch CM, Marcus J, Partilla JS, Rothman RB, Jacobson AE, Rice KC.
J Med Chem (2003) 46 : 1465 -1469
PubMed 12672246 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 6.41 7.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL416409 1 7.06
CHEMBL281594 VANOXERINE 3.0 1 6.90
CHEMBL289013 1 6.79
CHEMBL34032 1 6.77
CHEMBL409161 1 6.70
CHEMBL284096 1 6.69
CHEMBL34591 1 6.62
CHEMBL285673 1 6.62
CHEMBL36419 1 6.61
CHEMBL34372 1 6.61
CHEMBL35045 1 6.58
CHEMBL35411 1 6.43
CHEMBL290799 1 6.41
CHEMBL35122 1 6.36
CHEMBL36074 1 6.34
CHEMBL33902 1 6.28
CHEMBL36141 1 6.22
CHEMBL20648 1 6.04
CHEMBL33903 1 6.00
CHEMBL34697 1 5.67
CHEMBL35239 1 5.65
CHEMBL35005 1 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL416409 Ki = 88.0 nM 7.06
CHEMBL281594 VANOXERINE Ki = 126.0 nM 6.90
CHEMBL289013 Ki = 161.0 nM 6.79
CHEMBL34032 Ki = 171.0 nM 6.77
CHEMBL409161 Ki = 199.0 nM 6.70
CHEMBL284096 Ki = 205.0 nM 6.69
CHEMBL34591 Ki = 238.0 nM 6.62
CHEMBL285673 Ki = 239.0 nM 6.62
CHEMBL36419 Ki = 245.0 nM 6.61
CHEMBL34372 Ki = 248.0 nM 6.61
CHEMBL35045 Ki = 266.0 nM 6.58
CHEMBL35411 Ki = 370.0 nM 6.43
CHEMBL290799 Ki = 387.0 nM 6.41
CHEMBL35122 Ki = 442.0 nM 6.36
CHEMBL36074 Ki = 457.0 nM 6.34
CHEMBL33902 Ki = 531.0 nM 6.28
CHEMBL36141 Ki = 606.0 nM 6.22
CHEMBL20648 Ki = 902.0 nM 6.04
CHEMBL33903 Ki = 988.0 nM 6.00
CHEMBL34697 Ki = 2150.0 nM 5.67
CHEMBL35239 Ki = 2230.0 nM 5.65
CHEMBL35005 Ki = 2270.0 nM 5.64