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Assay Detail

CHEMBL4367996

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

Binding
Displacement of [3H]-citalopram from SERT in rat cortex tissue incubated for 60 mins by microbeta scintillation counting method
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis of new 5,6,7,8-tetrahydropyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT<sub>1A</sub> receptor ligands.
Ślifirski G, Król M, Kleps J, Podsadni P, Belka M, Bączek T, Siwek A, Stachowicz K, Szewczyk B, Nowak G, Bojarski A, Kozioł AE, Turło J, Herold F.
Eur J Med Chem (2019) 180 : 383 -397
PubMed 31325785 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 7.03 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4469537 1 8.10
CHEMBL4582567 1 7.82
CHEMBL11 IMIPRAMINE 4.0 1 7.54
CHEMBL4467024 1 7.54
CHEMBL4469633 1 7.51
CHEMBL4455658 1 7.47
CHEMBL4471395 1 7.28
CHEMBL4471755 1 7.23
CHEMBL4449982 1 7.22
CHEMBL4476164 1 7.15
CHEMBL4543669 1 7.14
CHEMBL4444099 1 7.11
CHEMBL4470437 1 7.06
CHEMBL4458712 1 7.01
CHEMBL4475730 1 6.98
CHEMBL4515025 1 6.96
CHEMBL4530671 1 6.93
CHEMBL4472972 1 6.88
CHEMBL4442394 1 6.88
CHEMBL4533362 1 6.84
CHEMBL4458537 1 6.82
CHEMBL4545518 1 6.67
CHEMBL4466243 1 6.62
CHEMBL4462825 1 6.60
CHEMBL4531647 1 6.52
CHEMBL4464118 1 6.51
CHEMBL4460224 1 6.22
CHEMBL4465006 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4469537 Ki = 8.0 nM 8.10
CHEMBL4582567 Ki = 15.0 nM 7.82
CHEMBL11 IMIPRAMINE Ki = 29.0 nM 7.54
CHEMBL4467024 Ki = 29.0 nM 7.54
CHEMBL4469633 Ki = 31.0 nM 7.51
CHEMBL4455658 Ki = 34.0 nM 7.47
CHEMBL4471395 Ki = 52.0 nM 7.28
CHEMBL4471755 Ki = 59.0 nM 7.23
CHEMBL4449982 Ki = 60.0 nM 7.22
CHEMBL4476164 Ki = 71.0 nM 7.15
CHEMBL4543669 Ki = 72.0 nM 7.14
CHEMBL4444099 Ki = 78.0 nM 7.11
CHEMBL4470437 Ki = 87.0 nM 7.06
CHEMBL4458712 Ki = 98.0 nM 7.01
CHEMBL4475730 Ki = 104.0 nM 6.98
CHEMBL4515025 Ki = 111.0 nM 6.96
CHEMBL4530671 Ki = 117.0 nM 6.93
CHEMBL4472972 Ki = 133.0 nM 6.88
CHEMBL4442394 Ki = 132.0 nM 6.88
CHEMBL4533362 Ki = 146.0 nM 6.84
CHEMBL4458537 Ki = 152.0 nM 6.82
CHEMBL4545518 Ki = 215.0 nM 6.67
CHEMBL4466243 Ki = 240.0 nM 6.62
CHEMBL4462825 Ki = 252.0 nM 6.60
CHEMBL4531647 Ki = 300.0 nM 6.52
CHEMBL4464118 Ki = 307.0 nM 6.51
CHEMBL4460224 Ki = 607.0 nM 6.22
CHEMBL4465006 Ki = 602.0 nM 6.22