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Assay Detail

CHEMBL672576

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

Binding
Binding affinity towards human Dopamine receptor D2 (short) by [3H]-spiperone displacement.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Enantio- and diastereocontrolled dopamine D1, D2, D3 and D4 receptor binding of N-(3-pyrrolidinylmethyl)benzamides synthesized from aspartic acid.
Thomas C, Hübner H, Gmeiner P.
Bioorg Med Chem Lett (1999) 9 : 841 -846
PubMed 10206547 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 6.43 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL354180 1 8.00
CHEMBL355566 1 7.68
CHEMBL168544 1 7.62
CHEMBL168611 1 7.55
CHEMBL267044 LEVOSULPIRIDE 2.0 1 7.29
CHEMBL169222 1 7.24
CHEMBL169193 1 7.10
CHEMBL166587 1 7.07
CHEMBL413343 1 6.92
CHEMBL424575 1 6.72
CHEMBL168566 1 6.27
CHEMBL168274 1 6.27
CHEMBL167414 1 6.19
CHEMBL423440 1 5.82
CHEMBL353090 1 5.80
CHEMBL168372 1 4.72
CHEMBL353087 1 4.68
CHEMBL167032 1 4.60
CHEMBL169631 1 4.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL354180 Ki = 10.0 nM 8.00
CHEMBL355566 Ki = 21.0 nM 7.68
CHEMBL168544 Ki = 24.0 nM 7.62
CHEMBL168611 Ki = 28.0 nM 7.55
CHEMBL267044 LEVOSULPIRIDE Ki = 51.0 nM 7.29
CHEMBL169222 Ki = 58.0 nM 7.24
CHEMBL169193 Ki = 79.0 nM 7.10
CHEMBL166587 Ki = 86.0 nM 7.07
CHEMBL413343 Ki = 120.0 nM 6.92
CHEMBL424575 Ki = 190.0 nM 6.72
CHEMBL168566 Ki = 540.0 nM 6.27
CHEMBL168274 Ki = 540.0 nM 6.27
CHEMBL167414 Ki = 640.0 nM 6.19
CHEMBL423440 Ki = 1500.0 nM 5.82
CHEMBL353090 Ki = 1600.0 nM 5.80
CHEMBL168372 Ki = 19000.0 nM 4.72
CHEMBL353087 Ki = 21000.0 nM 4.68
CHEMBL167032 Ki = 25000.0 nM 4.60
CHEMBL169631 Ki = 28000.0 nM 4.55