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Assay Detail

CHEMBL617533

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

Binding
Binding affinity against 5-hydroxytryptamine 2 receptor in rat using [3H]ketanserin as radioligand
31
Total Activities
31
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

Ketanserin analogues: structure-affinity relationships for 5-HT2 and 5-HT1C serotonin receptor binding.
Herndon JL, Ismaiel A, Ingher SP, Teitler M, Glennon RA.
J Med Chem (1992) 35 : 4903 -4910
PubMed 1479590 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 31 7.39 8.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL51 KETANSERIN 3.0 1 8.46
CHEMBL1202028 1 8.37
CHEMBL316004 LENPERONE 2.0 1 8.37
CHEMBL1788135 1 8.28
CHEMBL1744162 1 8.19
CHEMBL1203375 1 8.19
CHEMBL1788134 1 8.07
CHEMBL1202029 1 8.00
CHEMBL1202023 1 7.92
CHEMBL1202026 1 7.80
CHEMBL1202030 1 7.80
CHEMBL1202025 1 7.60
CHEMBL1744160 1 7.50
CHEMBL147995 1 6.90
CHEMBL1744163 1 6.75
CHEMBL147943 1 6.58
CHEMBL148189 1 6.37
CHEMBL1202027 1 6.19
CHEMBL1202024 1 6.18
CHEMBL1744161 1 6.18
CHEMBL344115 1 5.48
CHEMBL148005 1 -
CHEMBL1203377 1 -
CHEMBL113624 1 -
CHEMBL1744164 1 -
CHEMBL113600 1 -
CHEMBL278954 1 -
CHEMBL1203379 1 -
CHEMBL1203378 1 -
CHEMBL1203376 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL51 KETANSERIN Ki = 3.5 nM 8.46
CHEMBL1202028 Ki = 4.3 nM 8.37
CHEMBL316004 LENPERONE Ki = 4.3 nM 8.37
CHEMBL1788135 Ki = 5.3 nM 8.28
CHEMBL1744162 Ki = 6.5 nM 8.19
CHEMBL1203375 Ki = 6.5 nM 8.19
CHEMBL1788134 Ki = 8.5 nM 8.07
CHEMBL1202029 Ki = 10.0 nM 8.00
CHEMBL1202023 Ki = 12.0 nM 7.92
CHEMBL1202026 Ki = 16.0 nM 7.80
CHEMBL1202030 Ki = 16.0 nM 7.80
CHEMBL1202025 Ki = 25.0 nM 7.60
CHEMBL1744160 Ki = 32.0 nM 7.50
CHEMBL147995 Ki = 125.0 nM 6.90
CHEMBL1744163 Ki = 180.0 nM 6.75
CHEMBL147943 Ki = 260.0 nM 6.58
CHEMBL148189 Ki = 430.0 nM 6.37
CHEMBL1202027 Ki = 640.0 nM 6.19
CHEMBL1202024 Ki = 655.0 nM 6.18
CHEMBL1744161 Ki = 660.0 nM 6.18
CHEMBL344115 Ki = 3320.0 nM 5.48
CHEMBL148005 Ki > 10000.0 nM -
CHEMBL1203377 Ki > 10000.0 nM -
CHEMBL113624 Ki > 10000.0 nM -
CHEMBL1744164 Ki > 10000.0 nM -
CHEMBL113600 Ki > 10000.0 nM -
CHEMBL278954 Ki > 10000.0 nM -
CHEMBL1203379 Ki > 10000.0 nM -
CHEMBL1203378 Ki > 10000.0 nM -
CHEMBL1203376 Ki > 10000.0 nM -
CHEMBL144268 Ki > 10000.0 nM -