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Assay Detail

CHEMBL805340

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Binding
Binding affinity towards rat serotonin transporter (SERT)
51
Total Activities
51
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

Further exploration of 1-[2-[Bis-(4-fluorophenyl)methoxy]ethyl]piperazine (GBR 12909): role of N-aromatic, N-heteroaromatic, and 3-oxygenated N-phenylpropyl substituents on affinity for the dopamine and serotonin transporter.
Lewis D, Zhang Y, Prisinzano T, Dersch CM, Rothman RB, Jacobson AE, Rice KC.
Bioorg Med Chem Lett (2003) 13 : 1385 -1389
PubMed 12657288 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 51 6.48 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL29003 1 8.52
CHEMBL27748 1 8.52
CHEMBL286949 1 8.52
CHEMBL28660 1 7.52
CHEMBL29040 1 7.50
CHEMBL10914 1 7.30
CHEMBL29286 1 7.28
CHEMBL28414 1 7.24
CHEMBL28712 1 7.23
CHEMBL28907 1 7.16
CHEMBL283620 1 7.03
CHEMBL28505 1 7.00
CHEMBL31361 1 6.96
CHEMBL28867 1 6.96
CHEMBL417660 1 6.92
CHEMBL281594 VANOXERINE 3.0 1 6.90
CHEMBL286991 1 6.87
CHEMBL285566 1 6.82
CHEMBL282312 1 6.66
CHEMBL283662 1 6.66
CHEMBL28897 1 6.58
CHEMBL28236 1 6.47
CHEMBL416752 1 6.46
CHEMBL29065 1 6.36
CHEMBL283646 1 6.32
CHEMBL416198 1 6.32
CHEMBL416022 1 6.30
CHEMBL28876 1 6.28
CHEMBL28935 1 6.28
CHEMBL29151 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL29003 Ki = 3.0 nM 8.52
CHEMBL286949 Ki = 3.0 nM 8.52
CHEMBL27748 Ki = 3.0 nM 8.52
CHEMBL28660 Ki = 30.0 nM 7.52
CHEMBL29040 Ki = 32.0 nM 7.50
CHEMBL10914 Ki = 50.0 nM 7.30
CHEMBL29286 Ki = 53.0 nM 7.28
CHEMBL28414 Ki = 57.0 nM 7.24
CHEMBL28712 Ki = 59.0 nM 7.23
CHEMBL28907 Ki = 70.0 nM 7.16
CHEMBL283620 Ki = 93.0 nM 7.03
CHEMBL28505 Ki = 100.0 nM 7.00
CHEMBL28867 Ki = 110.0 nM 6.96
CHEMBL31361 Ki = 110.0 nM 6.96
CHEMBL417660 Ki = 120.0 nM 6.92
CHEMBL281594 VANOXERINE Ki = 126.0 nM 6.90
CHEMBL286991 Ki = 135.0 nM 6.87
CHEMBL285566 Ki = 150.0 nM 6.82
CHEMBL282312 Ki = 220.0 nM 6.66
CHEMBL283662 Ki = 220.0 nM 6.66
CHEMBL28897 Ki = 260.0 nM 6.58
CHEMBL28236 Ki = 340.0 nM 6.47
CHEMBL416752 Ki = 350.0 nM 6.46
CHEMBL29065 Ki = 440.0 nM 6.36
CHEMBL416198 Ki = 480.0 nM 6.32
CHEMBL283646 Ki = 480.0 nM 6.32
CHEMBL416022 Ki = 500.0 nM 6.30
CHEMBL28876 Ki = 530.0 nM 6.28
CHEMBL28935 Ki = 530.0 nM 6.28
CHEMBL29151 Ki = 580.0 nM 6.24
CHEMBL26320 Ki = 623.0 nM 6.21
CHEMBL28821 Ki = 700.0 nM 6.16
CHEMBL28598 Ki = 690.0 nM 6.16
CHEMBL28133 Ki = 920.0 nM 6.04
CHEMBL421862 Ki = 910.0 nM 6.04
CHEMBL29000 Ki = 970.0 nM 6.01
CHEMBL281669 Ki = 1050.0 nM 5.98
CHEMBL28726 Ki = 1130.0 nM 5.95
CHEMBL283837 Ki = 1240.0 nM 5.91
CHEMBL27907 Ki = 1310.0 nM 5.88
CHEMBL27626 Ki = 1360.0 nM 5.87
CHEMBL28947 Ki = 1360.0 nM 5.87
CHEMBL31571 Ki = 1940.0 nM 5.71
CHEMBL28191 Ki = 2200.0 nM 5.66
CHEMBL28306 Ki = 2600.0 nM 5.58
CHEMBL30257 Ki = 3300.0 nM 5.48
CHEMBL430537 Ki = 3300.0 nM 5.48
CHEMBL28125 Ki = 3300.0 nM 5.48
CHEMBL417305 Ki = 3900.0 nM 5.41
CHEMBL282821 Ki = 4100.0 nM 5.39