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Assay Detail

CHEMBL982080

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

Binding
Displacement of [3H]prazosin from adrenergic receptor alpha1 in CRL:CD(SD)BR-COBS rat brain cortex
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 6.95 7.78

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL477765 1 7.78
CHEMBL479231 1 7.70
CHEMBL476104 1 7.67
CHEMBL515334 1 7.66
CHEMBL477199 1 7.59
CHEMBL477200 1 7.48
CHEMBL477766 1 7.34
CHEMBL478394 1 7.33
CHEMBL476722 1 7.28
CHEMBL514074 1 7.11
CHEMBL476105 1 7.11
CHEMBL478413 1 7.11
CHEMBL517962 1 7.01
CHEMBL478412 1 6.90
CHEMBL8412 IPSAPIRONE 2.0 1 6.70
CHEMBL444988 1 6.68
CHEMBL477397 1 6.62
CHEMBL478411 1 6.60
CHEMBL476363 1 6.56
CHEMBL479026 1 6.48
CHEMBL514855 1 6.34
CHEMBL49 BUSPIRONE 4.0 1 6.22
CHEMBL479027 1 5.78
CHEMBL477828 1 5.72
CHEMBL477827 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL477765 Ki = 16.6 nM 7.78
CHEMBL479231 Ki = 20.0 nM 7.70
CHEMBL476104 Ki = 21.5 nM 7.67
CHEMBL515334 Ki = 21.9 nM 7.66
CHEMBL477199 Ki = 25.9 nM 7.59
CHEMBL477200 Ki = 33.2 nM 7.48
CHEMBL477766 Ki = 46.0 nM 7.34
CHEMBL478394 Ki = 46.7 nM 7.33
CHEMBL476722 Ki = 52.5 nM 7.28
CHEMBL514074 Ki = 78.0 nM 7.11
CHEMBL476105 Ki = 77.4 nM 7.11
CHEMBL478413 Ki = 77.7 nM 7.11
CHEMBL517962 Ki = 98.0 nM 7.01
CHEMBL478412 Ki = 127.0 nM 6.90
CHEMBL8412 IPSAPIRONE Ki = 200.0 nM 6.70
CHEMBL444988 Ki = 207.0 nM 6.68
CHEMBL477397 Ki = 240.0 nM 6.62
CHEMBL478411 Ki = 249.0 nM 6.60
CHEMBL476363 Ki = 276.0 nM 6.56
CHEMBL479026 Ki = 328.0 nM 6.48
CHEMBL514855 Ki = 457.0 nM 6.34
CHEMBL49 BUSPIRONE Ki = 600.0 nM 6.22
CHEMBL479027 Ki = 1651.0 nM 5.78
CHEMBL477828 Ki = 1915.0 nM 5.72
CHEMBL477827 Ki > 10000.0 nM -