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Assay Detail

CHEMBL875083

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

Binding
Binding affinity to 5-HT3 serotonin receptor in NG 108-15 neuroblastoma glioma cells using [3H]GR-65630 radioligand.
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Serotonin 3 (5-HT3) receptor (CHEMBL2094132)
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

The binding of arylguanidines at 5-HT(3) serotonin receptors: a structure-affinity investigation.
Dukat M, Choi YN, Teitler M, Du Pre A, Herrick-Davis K, Smith C, Glennon RA.
Bioorg Med Chem Lett (2001) 11 : 1599 -1603
PubMed 11412989 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 36 6.81 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL13535 1 9.15
CHEMBL40929 1 8.74
CHEMBL275293 1 8.57
CHEMBL40999 1 8.51
CHEMBL288055 1 8.30
CHEMBL41433 1 7.92
CHEMBL43078 1 7.85
CHEMBL13790 1 7.75
CHEMBL40567 1 7.75
CHEMBL13823 1 7.50
CHEMBL43298 1 7.44
CHEMBL42752 1 7.21
CHEMBL41853 1 6.72
CHEMBL840 4-CHLOROPHENYLBIGUANIDE 1 6.68
CHEMBL42538 1 6.66
CHEMBL40190 1 6.65
CHEMBL43961 1 6.64
CHEMBL44100 1 6.56
CHEMBL41040 1 6.49
CHEMBL43415 1 6.36
CHEMBL289594 1 6.35
CHEMBL289319 1 6.11
CHEMBL291064 1 6.05
CHEMBL297076 1 6.00
CHEMBL40488 1 5.92
CHEMBL13791 PHENYL BIGUANIDE 1 5.92
CHEMBL40459 1 5.90
CHEMBL43459 1 5.80
CHEMBL14047 PHENYLGUANIDINE 1 5.63
CHEMBL44236 1 5.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL13535 Ki = 0.7 nM 9.15
CHEMBL40929 Ki = 1.8 nM 8.74
CHEMBL275293 Ki = 2.7 nM 8.57
CHEMBL40999 Ki = 3.1 nM 8.51
CHEMBL288055 Ki = 5.0 nM 8.30
CHEMBL41433 Ki = 12.0 nM 7.92
CHEMBL43078 Ki = 14.0 nM 7.85
CHEMBL13790 Ki = 18.0 nM 7.75
CHEMBL40567 Ki = 18.0 nM 7.75
CHEMBL13823 Ki = 32.0 nM 7.50
CHEMBL43298 Ki = 36.0 nM 7.44
CHEMBL42752 Ki = 62.0 nM 7.21
CHEMBL41853 Ki = 190.0 nM 6.72
CHEMBL840 4-CHLOROPHENYLBIGUANIDE Ki = 210.0 nM 6.68
CHEMBL42538 Ki = 220.0 nM 6.66
CHEMBL40190 Ki = 225.0 nM 6.65
CHEMBL43961 Ki = 230.0 nM 6.64
CHEMBL44100 Ki = 274.0 nM 6.56
CHEMBL41040 Ki = 326.0 nM 6.49
CHEMBL43415 Ki = 442.0 nM 6.36
CHEMBL289594 Ki = 450.0 nM 6.35
CHEMBL289319 Ki = 780.0 nM 6.11
CHEMBL291064 Ki = 890.0 nM 6.05
CHEMBL297076 Ki = 990.0 nM 6.00
CHEMBL40488 Ki = 1200.0 nM 5.92
CHEMBL13791 PHENYL BIGUANIDE Ki = 1200.0 nM 5.92
CHEMBL40459 Ki = 1250.0 nM 5.90
CHEMBL43459 Ki = 1600.0 nM 5.80
CHEMBL14047 PHENYLGUANIDINE Ki = 2340.0 nM 5.63
CHEMBL44236 Ki = 2440.0 nM 5.61
CHEMBL42751 Ki = 2710.0 nM 5.57
CHEMBL41272 Ki = 6200.0 nM 5.21
CHEMBL295000 Ki = 6520.0 nM 5.19
CHEMBL40647 Ki > 10000.0 nM -
CHEMBL290199 Ki > 10000.0 nM -
CHEMBL14435 Ki > 10000.0 nM -