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Assay Detail

CHEMBL615400

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

Binding
Evaluated for binding affinity towards rat cortical membranes at 5-hydroxytryptamine 1 receptor binding site by using [3H]-5-HT as a radioligand.
42
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Serotonin 1 (5-HT1) receptor (CHEMBL2095159)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Central serotonin receptors as targets for drug research.
Glennon RA.
J Med Chem (1987) 30 : 1 -12
PubMed 3543362 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 42 5.95 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18785 RU-24969 1 8.70
CHEMBL39 SEROTONIN 3.0 1 8.70
CHEMBL8165 5-METHOXYTRYPTAMINE 1 8.70
CHEMBL19215 METERGOLINE 2.0 1 7.70
CHEMBL274866 1 7.70
CHEMBL7257 MEBUFOTENIN 2.0 1 7.30
CHEMBL500 PINDOLOL 4.0 1 7.00
CHEMBL267930 SPIPERONE 2.0 1 6.80
CHEMBL56 8-OH-DPAT 1 6.80
CHEMBL18772 QUIPAZINE 2.0 1 6.64
CHEMBL452861 LEVOPROPRANOLOL 2.0 1 6.52
CHEMBL1434583 1 6.04
CHEMBL8642 1 5.99
CHEMBL6437 MIANSERIN 4.0 1 5.96
CHEMBL18762 1 5.88
CHEMBL134519 2 5.64
CHEMBL16247 1 5.58
CHEMBL8600 DOM 1 5.54
CHEMBL8569 1 5.50
CHEMBL6607 BROLAMFETAMINE 2.0 1 5.48
CHEMBL267526 1 5.47
CHEMBL18786 CINANSERIN 2.0 1 5.46
CHEMBL16451 1 5.46
CHEMBL317634 1 5.45
CHEMBL19044 1 5.41
CHEMBL69700 2 5.38
CHEMBL1788248 1 5.37
CHEMBL8224 1 5.34
CHEMBL468880 1 5.30
CHEMBL405 AMPHETAMINE 4.0 1 5.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18785 RU-24969 Ki = 2.0 nM 8.70
CHEMBL8165 5-METHOXYTRYPTAMINE Ki = 2.0 nM 8.70
CHEMBL39 SEROTONIN Ki = 2.0 nM 8.70
CHEMBL19215 METERGOLINE Ki = 20.0 nM 7.70
CHEMBL274866 Ki = 20.0 nM 7.70
CHEMBL7257 MEBUFOTENIN Ki = 50.0 nM 7.30
CHEMBL500 PINDOLOL Ki = 100.0 nM 7.00
CHEMBL267930 SPIPERONE Ki = 160.0 nM 6.80
CHEMBL56 8-OH-DPAT Ki = 160.0 nM 6.80
CHEMBL18772 QUIPAZINE Ki = 230.0 nM 6.64
CHEMBL452861 LEVOPROPRANOLOL Ki = 300.0 nM 6.52
CHEMBL1434583 Ki = 920.0 nM 6.04
CHEMBL8642 Ki = 1020.0 nM 5.99
CHEMBL6437 MIANSERIN Ki = 1100.0 nM 5.96
CHEMBL18762 Ki = 1320.0 nM 5.88
CHEMBL134519 Ki = 2290.0 nM 5.64
CHEMBL134519 Ki = 2300.0 nM 5.64
CHEMBL16247 Ki = 2660.0 nM 5.58
CHEMBL8600 DOM Ki = 2890.0 nM 5.54
CHEMBL8569 Ki = 3170.0 nM 5.50
CHEMBL6607 BROLAMFETAMINE Ki = 3340.0 nM 5.48
CHEMBL267526 Ki = 3370.0 nM 5.47
CHEMBL16451 Ki = 3500.0 nM 5.46
CHEMBL18786 CINANSERIN Ki = 3500.0 nM 5.46
CHEMBL317634 Ki = 3550.0 nM 5.45
CHEMBL19044 Ki = 3870.0 nM 5.41
CHEMBL69700 Ki = 4200.0 nM 5.38
CHEMBL69700 Ki = 4200.0 nM 5.38
CHEMBL1788248 Ki = 4300.0 nM 5.37
CHEMBL8224 Ki = 4570.0 nM 5.34
CHEMBL468880 Ki = 5000.0 nM 5.30
CHEMBL405 AMPHETAMINE Ki = 7660.0 nM 5.12
CHEMBL1927025 Ki = 13000.0 nM 4.89
CHEMBL1788278 Ki = 13200.0 nM 4.88
CHEMBL8301 Ki = 14100.0 nM 4.85
CHEMBL8389 Ki = 46400.0 nM 4.33
CHEMBL277540 Ki = 64600.0 nM 4.19
CHEMBL278663 PARA-METHOXYAMPHETAMINE Ki = 79400.0 nM 4.10
CHEMBL18331 PIRENPERONE Ki - nM -
CHEMBL12314 MESULERGINE Ki - nM -
CHEMBL51 KETANSERIN Ki - nM -
CHEMBL478 CHLOROPHENYLPIPERAZINE Ki - nM -