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Assay Detail

CHEMBL982079

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

Binding
Displacement of [3H]8-OH-DPAT from 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Hippocampus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 1A (CHEMBL273)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis of new arylpiperazinylalkylthiobenzimidazole, benzothiazole, or benzoxazole derivatives as potent and selective 5-HT1A serotonin receptor ligands.
Siracusa MA, Salerno L, Modica MN, Pittalà V, Romeo G, Amato ME, Nowak M, Bojarski AJ, Mereghetti I, Cagnotto A, Mennini T.
J Med Chem (2008) 51 : 4529 -4538
PubMed 18598015 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 8.35 10.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL514074 1 10.03
CHEMBL477765 1 9.57
CHEMBL479231 1 9.57
CHEMBL477200 1 9.54
CHEMBL476722 1 9.28
CHEMBL476104 1 9.26
CHEMBL478413 1 9.11
CHEMBL478394 1 9.06
CHEMBL477199 1 9.00
CHEMBL515334 1 9.00
CHEMBL477766 1 8.89
CHEMBL517962 1 8.80
CHEMBL479026 1 8.60
CHEMBL8412 IPSAPIRONE 2.0 1 8.26
CHEMBL478411 1 8.02
CHEMBL478412 1 7.85
CHEMBL479027 1 7.83
CHEMBL49 BUSPIRONE 4.0 1 7.82
CHEMBL476105 1 7.78
CHEMBL444988 1 7.51
CHEMBL477397 1 7.48
CHEMBL476363 1 7.17
CHEMBL514855 1 7.02
CHEMBL477828 1 6.49
CHEMBL477827 1 5.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL514074 Ki = 0.094 nM 10.03
CHEMBL477765 Ki = 0.27 nM 9.57
CHEMBL479231 Ki = 0.27 nM 9.57
CHEMBL477200 Ki = 0.29 nM 9.54
CHEMBL476722 Ki = 0.52 nM 9.28
CHEMBL476104 Ki = 0.55 nM 9.26
CHEMBL478413 Ki = 0.78 nM 9.11
CHEMBL478394 Ki = 0.88 nM 9.06
CHEMBL477199 Ki = 1.0 nM 9.00
CHEMBL515334 Ki = 1.0 nM 9.00
CHEMBL477766 Ki = 1.3 nM 8.89
CHEMBL517962 Ki = 1.6 nM 8.80
CHEMBL479026 Ki = 2.5 nM 8.60
CHEMBL8412 IPSAPIRONE Ki = 5.5 nM 8.26
CHEMBL478411 Ki = 9.6 nM 8.02
CHEMBL478412 Ki = 14.1 nM 7.85
CHEMBL479027 Ki = 14.9 nM 7.83
CHEMBL49 BUSPIRONE Ki = 15.0 nM 7.82
CHEMBL476105 Ki = 16.6 nM 7.78
CHEMBL444988 Ki = 31.2 nM 7.51
CHEMBL477397 Ki = 33.1 nM 7.48
CHEMBL476363 Ki = 67.2 nM 7.17
CHEMBL514855 Ki = 95.2 nM 7.02
CHEMBL477828 Ki = 326.0 nM 6.49
CHEMBL477827 Ki = 1702.0 nM 5.77