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Assay Detail

CHEMBL617013

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Binding
Binding affinity towards 5-hydroxytryptamine 2 receptor using [3H]-ketanserin as radioligand.
ChEMBL ↗
51
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Serotonin 2 (5-HT2) receptor (CHEMBL2093870) ↗
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Three-dimensional quantitative structure-activity relationships of 5-HT receptor binding data for tetrahydropyridinylindole derivatives: a comparison of the Hansch and CoMFA methods.
Agarwal A, Pearson PP, Taylor EW, Li HB, Dahlgren T, Herslöf M, Yang Y, Lambert G, Nelson DL, Regan JW.
J Med Chem (1993) 36 : 4006 -4014
PubMed 8258822 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 51 6.10 7.81

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL281937 — — 1 7.81
CHEMBL341485 — — 1 7.71
CHEMBL285157 — — 1 7.36
CHEMBL27025 — — 1 7.35
CHEMBL27227 — — 1 7.32
CHEMBL283185 — — 1 7.29
CHEMBL26655 — — 1 7.17
CHEMBL283416 — — 1 7.06
CHEMBL287576 — — 1 6.92
CHEMBL442534 — — 1 6.90
CHEMBL26921 — — 1 6.84
CHEMBL283257 — — 1 6.79
CHEMBL340175 — — 1 6.70
CHEMBL27811 — — 1 6.69
CHEMBL436568 — — 1 6.67
CHEMBL128288 — — 1 6.66
CHEMBL337381 — — 1 6.54
CHEMBL26836 — — 1 6.45
CHEMBL283397 — — 1 6.40
CHEMBL27998 — — 1 6.25
CHEMBL128544 — — 1 6.23
CHEMBL26850 — — 1 6.06
CHEMBL285777 — — 1 6.05
CHEMBL18785 RU-24969 — 1 6.04
CHEMBL283899 — — 1 6.02
CHEMBL281716 — — 1 6.02
CHEMBL27643 — — 1 6.01
CHEMBL417470 — — 1 5.97
CHEMBL284107 — — 1 5.96
CHEMBL26972 — — 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL281937 — Ki = 15.49 nM 7.81
CHEMBL341485 — Ki = 19.32 nM 7.71
CHEMBL285157 — Ki = 43.55 nM 7.36
CHEMBL27025 — Ki = 44.77 nM 7.35
CHEMBL27227 — Ki = 47.86 nM 7.32
CHEMBL283185 — Ki = 51.05 nM 7.29
CHEMBL26655 — Ki = 66.99 nM 7.17
CHEMBL283416 — Ki = 86.5 nM 7.06
CHEMBL287576 — Ki = 119.95 nM 6.92
CHEMBL442534 — Ki = 125.89 nM 6.90
CHEMBL26921 — Ki = 145.88 nM 6.84
CHEMBL283257 — Ki = 164.06 nM 6.79
CHEMBL340175 — Ki = 199.53 nM 6.70
CHEMBL27811 — Ki = 203.7 nM 6.69
CHEMBL436568 — Ki = 213.8 nM 6.67
CHEMBL128288 — Ki = 218.78 nM 6.66
CHEMBL337381 — Ki = 286.42 nM 6.54
CHEMBL26836 — Ki = 354.81 nM 6.45
CHEMBL283397 — Ki = 398.11 nM 6.40
CHEMBL27998 — Ki = 557.19 nM 6.25
CHEMBL128544 — Ki = 591.56 nM 6.23
CHEMBL26850 — Ki = 868.96 nM 6.06
CHEMBL285777 — Ki = 897.43 nM 6.05
CHEMBL18785 RU-24969 Ki = 912.01 nM 6.04
CHEMBL281716 — Ki = 957.19 nM 6.02
CHEMBL283899 — Ki = 954.99 nM 6.02
CHEMBL27643 — Ki = 984.01 nM 6.01
CHEMBL417470 — Ki = 1078.95 nM 5.97
CHEMBL284107 — Ki = 1104.08 nM 5.96
CHEMBL26972 — Ki = 1288.25 nM 5.89
CHEMBL281434 — Ki = 1348.96 nM 5.87
CHEMBL25812 — Ki = 1445.44 nM 5.84
CHEMBL130159 — Ki = 1479.11 nM 5.83
CHEMBL539159 — Ki = 1690.44 nM 5.77
CHEMBL287441 — Ki = 1729.82 nM 5.76
CHEMBL28105 — Ki = 2421.03 nM 5.62
CHEMBL26900 — Ki = 2805.43 nM 5.55
CHEMBL282799 — Ki = 2904.02 nM 5.54
CHEMBL280779 — Ki = 3097.42 nM 5.51
CHEMBL27719 — Ki = 3630.78 nM 5.44
CHEMBL26311 — Ki = 4365.16 nM 5.36
CHEMBL284447 — Ki = 4365.16 nM 5.36
CHEMBL131203 — Ki = 5000.35 nM 5.30
CHEMBL286264 — Ki = 5116.82 nM 5.29
CHEMBL281432 — Ki = 5128.61 nM 5.29
CHEMBL287655 — Ki = 6309.57 nM 5.20
CHEMBL26322 — Ki = 10000.0 nM 5.00
CHEMBL26868 — Ki = 10789.47 nM 4.97
CHEMBL283398 — Ki = 16826.74 nM 4.77
CHEMBL287097 — Ki = 50003.45 nM 4.30