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Assay Detail

CHEMBL840215

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Binding
Inhibition constant against [3H]-spiperone binding to human Dopamine receptor D3 expressed in CHO cells
ChEMBL ↗
52
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(3) dopamine receptor (CHEMBL234) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists.
Boeckler F, Ohnmacht U, Lehmann T, Utz W, Hübner H, Gmeiner P.
J Med Chem (2005) 48 : 2493 -2508
PubMed 15801839 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 52 6.66 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL157138 LISURIDE 3.0 1 9.85
CHEMBL301265 PRAMIPEXOLE 4.0 1 9.14
CHEMBL301559 — — 1 9.10
CHEMBL531 PERGOLIDE 4.0 1 9.07
CHEMBL155731 QUINELORANE 2.0 1 9.03
CHEMBL70565 — — 1 8.85
CHEMBL189438 — — 1 8.46
CHEMBL316983 — — 1 8.28
CHEMBL372020 — — 1 8.14
CHEMBL189486 — — 1 7.64
CHEMBL240773 QUINPIROLE 2.0 1 7.62
CHEMBL7549 PRECLAMOL 2.0 1 7.60
CHEMBL364916 — — 1 7.51
CHEMBL192795 — — 1 7.41
CHEMBL192746 — — 1 7.36
CHEMBL190679 — — 1 7.34
CHEMBL372854 — — 1 7.31
CHEMBL190519 — — 1 7.23
CHEMBL189880 — — 1 7.22
CHEMBL193170 — — 1 7.06
CHEMBL193776 — — 1 6.58
CHEMBL95618 — — 1 6.49
CHEMBL191938 — — 1 6.49
CHEMBL96958 — — 1 6.38
CHEMBL95230 — — 1 6.38
CHEMBL97319 — — 1 6.30
CHEMBL192037 — — 1 6.24
CHEMBL440143 — — 1 6.21
CHEMBL97283 — — 1 6.17
CHEMBL99291 — — 1 6.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL157138 LISURIDE Ki = 0.1413 nM 9.85
CHEMBL301265 PRAMIPEXOLE Ki = 0.7244 nM 9.14
CHEMBL301559 — Ki = 0.7943 nM 9.10
CHEMBL531 PERGOLIDE Ki = 0.8511 nM 9.07
CHEMBL155731 QUINELORANE Ki = 0.9333 nM 9.03
CHEMBL70565 — Ki = 1.413 nM 8.85
CHEMBL189438 — Ki = 3.467 nM 8.46
CHEMBL316983 — Ki = 5.248 nM 8.28
CHEMBL372020 — Ki = 7.244 nM 8.14
CHEMBL189486 — Ki = 22.91 nM 7.64
CHEMBL240773 QUINPIROLE Ki = 23.99 nM 7.62
CHEMBL7549 PRECLAMOL Ki = 25.12 nM 7.60
CHEMBL364916 — Ki = 30.9 nM 7.51
CHEMBL192795 — Ki = 38.9 nM 7.41
CHEMBL192746 — Ki = 43.65 nM 7.36
CHEMBL190679 — Ki = 45.71 nM 7.34
CHEMBL372854 — Ki = 48.98 nM 7.31
CHEMBL190519 — Ki = 58.88 nM 7.23
CHEMBL189880 — Ki = 60.26 nM 7.22
CHEMBL193170 — Ki = 87.1 nM 7.06
CHEMBL193776 — Ki = 263.03 nM 6.58
CHEMBL95618 — Ki = 323.59 nM 6.49
CHEMBL191938 — Ki = 323.59 nM 6.49
CHEMBL96958 — Ki = 416.87 nM 6.38
CHEMBL95230 — Ki = 416.87 nM 6.38
CHEMBL97319 — Ki = 501.19 nM 6.30
CHEMBL192037 — Ki = 575.44 nM 6.24
CHEMBL440143 — Ki = 616.6 nM 6.21
CHEMBL97283 — Ki = 676.08 nM 6.17
CHEMBL99291 — Ki = 724.44 nM 6.14
CHEMBL98072 — Ki = 794.33 nM 6.10
CHEMBL323557 — Ki = 912.01 nM 6.04
CHEMBL98071 — Ki = 1412.54 nM 5.85
CHEMBL97750 — Ki = 1445.44 nM 5.84
CHEMBL363608 — Ki = 1548.82 nM 5.81
CHEMBL318924 — Ki = 1659.59 nM 5.78
CHEMBL97436 — Ki = 1819.7 nM 5.74
CHEMBL192906 — Ki = 1905.46 nM 5.72
CHEMBL189834 — Ki = 2089.3 nM 5.68
CHEMBL193304 — Ki = 2398.83 nM 5.62
CHEMBL364737 — Ki = 2511.89 nM 5.60
CHEMBL192709 — Ki = 2818.38 nM 5.55
CHEMBL193077 — Ki = 2818.38 nM 5.55
CHEMBL98563 — Ki = 3630.78 nM 5.44
CHEMBL190542 — Ki = 3630.78 nM 5.44
CHEMBL192433 — Ki = 4365.16 nM 5.36
CHEMBL365960 — Ki = 4786.3 nM 5.32
CHEMBL193043 — Ki = 6025.6 nM 5.22
CHEMBL192501 — Ki = 7943.28 nM 5.10
CHEMBL97348 — Ki = 8511.38 nM 5.07