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Assay Detail

CHEMBL4316413

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

Binding
Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Virtual screening-driven discovery of dual 5-HT<sub>6</sub>/5-HT<sub>2A</sub> receptor ligands with pro-cognitive properties.
Staroń J, Kurczab R, Warszycki D, Satała G, Krawczyk M, Bugno R, Lenda T, Popik P, Hogendorf AS, Hogendorf A, Dubiel K, Matłoka M, Moszczyński-Pętkowski R, Pieczykolan J, Wieczorek M, Zajdel P, Bojarski AJ.
Eur J Med Chem (2020) 185 : 111857 -111857
PubMed 31734022 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 6.46 7.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL49 BUSPIRONE 4.0 1 7.46
CHEMBL4435528 1 7.19
CHEMBL4464881 1 7.04
CHEMBL4583082 1 6.92
CHEMBL4462814 1 6.90
CHEMBL4591410 1 6.84
CHEMBL4584504 1 6.70
CHEMBL4593671 1 6.66
CHEMBL4465414 1 6.54
CHEMBL4519266 1 6.48
CHEMBL4438434 1 6.40
CHEMBL4442111 1 6.37
CHEMBL4474618 1 6.13
CHEMBL4552041 1 6.11
CHEMBL4437523 1 6.00
CHEMBL4448285 1 5.98
CHEMBL3286580 IDALOPIRDINE 3.0 1 5.41
CHEMBL4442855 1 5.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL49 BUSPIRONE Ki = 34.3 nM 7.46
CHEMBL4435528 Ki = 64.0 nM 7.19
CHEMBL4464881 Ki = 91.0 nM 7.04
CHEMBL4583082 Ki = 120.0 nM 6.92
CHEMBL4462814 Ki = 125.0 nM 6.90
CHEMBL4591410 Ki = 146.0 nM 6.84
CHEMBL4584504 Ki = 202.0 nM 6.70
CHEMBL4593671 Ki = 218.0 nM 6.66
CHEMBL4465414 Ki = 292.0 nM 6.54
CHEMBL4519266 Ki = 334.0 nM 6.48
CHEMBL4438434 Ki = 399.0 nM 6.40
CHEMBL4442111 Ki = 431.0 nM 6.37
CHEMBL4474618 Ki = 732.0 nM 6.13
CHEMBL4552041 Ki = 775.0 nM 6.11
CHEMBL4437523 Ki = 1010.0 nM 6.00
CHEMBL4448285 Ki = 1052.0 nM 5.98
CHEMBL3286580 IDALOPIRDINE Ki = 3936.0 nM 5.41
CHEMBL4442855 Ki = 6204.0 nM 5.21