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D2 receptor

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Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 215

Nomenclature: D2 receptor

Family: Dopamine receptors

Contents:

Gene and Protein Information Click here for help
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 443 11q23.2 DRD2 dopamine receptor D2 9,45
Mouse 7 444 9 26.72 cM Drd2 dopamine receptor D2 88
Rat 7 444 8q23 Drd2 dopamine receptor D2 9,24
Gene and Protein Information Comments
The human D2 receptor exists as two alternatively spliced isoforms [44]. The 443 amino acid receptor is the long form (D2L). The short form (D2S) is 414 amino acids long.
Previous and Unofficial Names Click here for help
D2A and D2B | dopamine D2 receptor | dopamine receptor 2 | D2R | D2 receptor | D2(415) and D2(444)
Database Links Click here for help
Specialist databases
GPCRdb drd2_human (Hs), drd2_mouse (Mm), drd2_rat (Rn)
Other databases
Alphafold P14416 (Hs), P61168 (Mm), P61169 (Rn)
ChEMBL Target CHEMBL217 (Hs), CHEMBL3427 (Mm), CHEMBL339 (Rn)
DrugBank Target P14416 (Hs)
Ensembl Gene ENSG00000149295 (Hs), ENSMUSG00000032259 (Mm), ENSRNOG00000008428 (Rn)
Entrez Gene 1813 (Hs), 13489 (Mm), 24318 (Rn)
Human Protein Atlas ENSG00000149295 (Hs)
KEGG Gene hsa:1813 (Hs), mmu:13489 (Mm), rno:24318 (Rn)
OMIM 126450 (Hs)
Orphanet ORPHA121177 (Hs)
Pharos P14416 (Hs)
RefSeq Nucleotide NM_000795 (Hs), NM_010077 (Mm), NM_012547 (Rn)
RefSeq Protein NP_000786 (Hs), NP_034207 (Mm), NP_036679 (Rn)
UniProtKB P14416 (Hs), P61168 (Mm), P61169 (Rn)
Wikipedia DRD2 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Structure of the D2 dopamine receptor bound to the atypical antipsychotic drug risperidone
PDB Id:  6CM4
Ligand:  risperidone
Resolution:  2.9Å
Species:  Human
References:  132
Natural/Endogenous Ligands Click here for help
dopamine

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
rotigotine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Agonist 10.2 pKi 37
⤷ pKi 10.2 (Ki 6x10-11 M) [37]
aripiprazole Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Partial agonist 9.7 pKi 104
⤷ pKi 9.7 [104]
brexpiprazole Small molecule or natural product Approved drug Hs Partial agonist 9.5 pKi 76
⤷ pKi 9.5 (Ki 3x10-10 M) [76]
lisuride Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 9.2 – 9.5 pKi 86
⤷ pKi 9.2 – 9.5 [86]
aripiprazole Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 9.1 pKi 138
⤷ pKi 9.1 (Ki 8x10-10 M) [138]
cabergoline Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Partial agonist 9.0 – 9.2 pKi 86
⤷ pKi 9.0 – 9.2 [86]
terguride Small molecule or natural product Approved drug Click here for species-specific activity table Hs Partial agonist 9.1 pKi 86
⤷ pKi 9.1 [86]
roxindole Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 8.6 pKi 86
⤷ pKi 8.6 [86]
UNC9975 Small molecule or natural product Hs Biased agonist 8.6 pKi 3
⤷ pKi 8.6 (Ki 2.6x10-9 M) [3]
Description: β-arrestin 2 biased agonist.
UNC0006 Small molecule or natural product Hs Biased agonist 8.3 pKi 3
⤷ pKi 8.3 (Ki 5x10-9 M) [3]
Description: β-arrestin 2 biased agonist.
cariprazine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 8.2 pKi 1
⤷ pKi 8.2 (Ki 5.7x10-9 M) [1]
Description: Binding affinity to human dopamine D2L receptor
MLS1547 Small molecule or natural product Hs Biased agonist 8.2 pKi 40
⤷ pKi 8.2 (Ki 5.9x10-9 M) [40]
Description: Biased agonist for G-protein coupling to Gi.
(-)-N-porphynorapomorphine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.5 – 8.9 pKi 41,102
⤷ pKi 7.5 – 8.9 [41,102]
ropinirole Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Agonist 8.1 pKi 49
⤷ pKi 8.1 (Ki 7.2x10-9 M) [49]
LP-44 Small molecule or natural product Click here for species-specific activity table Hs Agonist 8.1 pKi 71
⤷ pKi 8.1 (Ki 7.3x10-9 M) [71]
sumanirole Small molecule or natural product Hs Full agonist 8.1 pKi 83
⤷ pKi 8.1 (Ki 9x10-9 M) [83]
bromocriptine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 7.3 – 8.3 pKi 41,86,102
⤷ pKi 7.3 – 8.3 [41,86,102]
apomorphine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Partial agonist 7.6 pKi 120
⤷ pKi 7.6 [120]
pergolide Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 7.5 – 7.6 pKi 86
⤷ pKi 7.5 – 7.6 [86]
bromocriptine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Partial agonist 7.3 pKi 120
⤷ pKi 7.3 [120]
UNC9994 Small molecule or natural product Hs Biased agonist 7.1 pKi 3
⤷ pKi 7.1 (Ki 7.9x10-8 M) [3]
Description: β-arrestin 2 biased agonist.
compound 3 [PMID: 23134120] Small molecule or natural product Click here for species-specific activity table Hs Agonist 6.9 pKi 121
⤷ pKi 6.9 (Ki 1.18x10-7 M) [121]
piribedil Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 6.8 – 6.9 pKi 86
⤷ pKi 6.8 – 6.9 [86]
LP-211 Small molecule or natural product Click here for species-specific activity table Hs Agonist 6.8 pKi 72
⤷ pKi 6.8 (Ki 1.42x10-7 M) [72]
LP-12 Small molecule or natural product Click here for species-specific activity table Hs Agonist 6.7 pKi 71
⤷ pKi 6.7 (Ki 2.24x10-7 M) [71]
apomorphine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 5.7 – 7.5 pKi 25,41,86,102,118
⤷ pKi 5.7 – 7.5 [25,41,86,102,118]
7-OH-DPAT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.6 – 7.6 pKi 25,41,75
⤷ pKi 5.6 – 7.6 [25,41,75]
HS665 Small molecule or natural product Click here for species-specific activity table Hs Agonist 6.3 pKi 121
⤷ pKi 6.3 (Ki 4.5x10-7 M) [121]
quinpirole Small molecule or natural product Click here for species-specific activity table Hs Full agonist 4.9 – 7.7 pKi 25,85,92,118,120,129
⤷ pKi 4.9 – 7.7 [25,85,92,118,120,129]
pramipexole Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 5.1 – 7.4 pKi 85,102
⤷ pKi 5.1 – 7.4 [85,102]
7-OH-DPAT Small molecule or natural product Rn Full agonist 6.2 pKi 33
⤷ pKi 6.2 [33]
dopamine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Immunopharmacology Ligand Hs Full agonist 4.7 – 7.2 pKi 25,41,102
⤷ pKi 4.7 – 7.2 [25,41,102]
PD 128907 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.4 – 6.4 pKi 94,102
⤷ pKi 5.4 – 6.4 [94,102]
dopamine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Immunopharmacology Ligand Rn Full agonist 5.3 – 6.4 pKi 104,120
⤷ pKi 5.3 – 6.4 [104,120]
7-trans-OH-PIPAT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.6 pKi 33
⤷ pKi 5.6 [33]
quinelorane Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.5 – 5.7 pKi 87,118
⤷ pKi 5.5 – 5.7 [87,118]
benzquinamide Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Agonist 5.4 pKi 46
⤷ pKi 5.4 (Ki 3.964x10-6 M) [46]
quinpirole Small molecule or natural product Click here for species-specific activity table Rn Full agonist 5.2 pKi 120
⤷ pKi 5.2 [120]
UNC9975 Small molecule or natural product Hs Biased agonist 9.0 pEC50 3
⤷ pEC50 9.0 (EC50 1.1x10-9 M) [3]
Description: This compound shows biased agonism towards D2-mediated β-arrestin-2 translocation measured using the Tango assay.
UNC0006 Small molecule or natural product Hs Biased agonist 8.9 pEC50 3
⤷ pEC50 8.9 (EC50 1.2x10-9 M) [3]
Description: Biased agonist of D2-mediated β-arrestin-2 translocation measured using the Tango assay.
UNC9994 Small molecule or natural product Hs Biased agonist 8.2 pEC50 3
⤷ pEC50 8.2 (EC50 6.1x10-9 M) [3]
Description: This compound shows biased agonism towards D2-mediated β-arrestin-2 translocation measured using the Tango assay.
aripiprazole Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 7.4 pEC50 3
⤷ pEC50 7.4 (EC50 3.8x10-8 M) [3]
Description: Measuring cAMP production via the Gi-coupled signaling pathway
vilazodone Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Agonist 6.2 pIC50 51
⤷ pIC50 6.2 (IC50 6.66x10-7 M) [51]
View species-specific agonist tables
Agonist Comments
Terguride and roxindole have been reported to be partial agonists at the D2S receptor and antagonists at the D2L receptor.
Although benzquinamide has higher affinity for α-adrenoceptors, it is suggested in [46] that it is more likely that drug-induced modulation of D2 receptor activity is responsible for the drug's antiemetic action.
Allosteric modulation of the D2 receptor by SB269652 only occurs when D2 receptor dimers form, with the ligand assuming a 'bitopic' pose and interacting with different sites on each of the two protomers in the dimer [70].
UNC0006, UNC9994 and UNC9975 are partial biased agonists of β-arrestin 2 recruitment at the D2 receptor as measured using three different assays (β-arrestin-2 translocation Tango assay, DiscoveRx assay and BRET-based β-arrestin-2 recruitment assay) [3]. Tango assay pEC50 values and binding Kis are provided in the table above.
G protein-biased, cariprazine-based partial agonists are reported in [115].
Antagonists
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Ligand Sp. Action Value Parameter Reference
[3H]nemonapride Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Ligand has a PDB structure Hs Antagonist 10.9 pKd 77
⤷ pKd 10.9 [77]
[3H]spiperone Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Ligand has a PDB structure Rn Antagonist 10.2 pKd 24,52,141
⤷ pKd 10.2 (Kd 5.7x10-11 M) [24,52,141]
[3H]raclopride Small molecule or natural product Ligand is labelled Ligand is radioactive Rn Antagonist 8.9 pKd 67
⤷ pKd 8.9 (Kd 1.2x10-9 M) [67]
[3H]N-methylspiperone Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Rn Antagonist 10.7 pKi 104
⤷ pKi 10.7 [104]
benperidol Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 10.6 pKi 111
⤷ pKi 10.6 (Ki 2.7x10-11 M) [111]
blonanserin Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 9.9 pKi 90
⤷ pKi 9.9 (Ki 1.4x10-10 M) [90]
pipotiazine Small molecule or natural product Approved drug Primary target of this compound Hs Antagonist 9.7 pKi 119
⤷ pKi 9.7 (Ki 2x10-10 M) [119]
risperidone Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 9.4 pKi 11
⤷ pKi 9.4 (Ki 4.4x10-10 M) [11]
perphenazine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 8.9 – 9.6 pKi 64,108
⤷ pKi 8.9 – 9.6 (Ki 1.4x10-9 – 2.6x10-10 M) [64,108]
perospirone Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 9.2 pKi 109
⤷ pKi 9.2 (Ki 6x10-10 M) [109]
eticlopride Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 9.2 pKi 75,125
⤷ pKi 9.2 [75,125]
trifluoperazine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 8.9 – 9.0 pKi 64,110
⤷ pKi 8.9 – 9.0 (Ki 1.3x10-9 – 9.6x10-10 M) [64,110]
asenapine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 8.9 pKi 114
⤷ pKi 8.9 (Ki 1.2x10-9 M) [114]
terguride Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 8.9 pKi 86
⤷ pKi 8.9 [86]
spiperone Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 8.4 – 9.4 pKi 75,87,120,125
⤷ pKi 8.4 – 9.4 [75,87,120,125]
fluphenazine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 8.8 pKi 101
⤷ pKi 8.8 (Ki 1.44x10-9 M) [101]
flupentixol Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 8.8 pKi 41
⤷ pKi 8.8 (Ki 1.5x10-9 M) [41]
nafadotride Small molecule or natural product Click here for species-specific activity table Rn Antagonist 8.8 pKi 104
⤷ pKi 8.8 [104]
lurasidone Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 8.8 pKi 55
⤷ pKi 8.8 (Ki 1.68x10-9 M) [55]
olanzapine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 8.7 pKi 11
⤷ pKi 8.7 (Ki 2.1x10-9 M) [11]
mesoridazine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 8.7 pKi 32
⤷ pKi 8.7 (Ki 2.2x10-9 M) [32]
roxindole Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.6 pKi 86
⤷ pKi 8.6 [86]
ziprasidone Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 8.6 pKi 11
⤷ pKi 8.6 (Ki 2.8x10-9 M) [11]
chlorprothixene Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 8.5 pKi 130
⤷ pKi 8.5 (Ki 2.96x10-9 M) [130]
nafadotride Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.5 pKi 103
⤷ pKi 8.5 [103]
raclopride Small molecule or natural product Click here for species-specific activity table Rn Antagonist 7.7 – 9.3 pKi 104,120
⤷ pKi 7.7 – 9.3 [104,120]
domperidone Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 8.5 pKi 120
⤷ pKi 8.5 [120]
sertindole Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 8.0 – 8.9 pKi 63-64,108
⤷ pKi 8.0 – 8.9 (Ki 9.1x10-9 – 1.2x10-9 M) [63-64,108]
prochlorperazine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 8.4 pKi 13
⤷ pKi 8.4 (Ki 3.61x10-9 M) [13]
haloperidol Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 8.3 pKi 120
⤷ pKi 8.3 [120]
(+)-sulpiride Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.2 pKi 41
⤷ pKi 8.2 (Ki 6x10-9 M) [41]
L-741,626 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.9 – 8.5 pKi 47,66
⤷ pKi 7.9 – 8.5 [47,66]
domperidone Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 7.9 – 8.4 pKi 41,118
⤷ pKi 7.9 – 8.4 (Ki 1.26x10-8 – 3.98x10-9 M) [41,118]
loxapine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 7.9 – 8.3 pKi 64,110
⤷ pKi 7.9 – 8.3 (Ki 1.2x10-8 – 5x10-9 M) [64,110]
(+)-butaclamol Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.5 – 8.7 pKi 25,41,75,125
⤷ pKi 7.5 – 8.7 [25,41,75,125]
haloperidol Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.4 – 8.8 pKi 41,75,85,118,126
⤷ pKi 7.4 – 8.8 [41,75,85,118,126]
raclopride Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.0 pKi 87
⤷ pKi 8.0 (Ki 1x10-8 M) [87]
zotepine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 8.0 pKi 107
⤷ pKi 8.0 (Ki 1.1x10-8 M) [107]
(-)-stepholidine Small molecule or natural product Hs Antagonist 7.9 pKi 84
⤷ pKi 7.9 (Ki 1.16x10-8 M) [84]
pimozide Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.0 – 8.8 pKi 41,118
⤷ pKi 7.0 – 8.8 [41,118]
amisulpride Small molecule or natural product Approved drug Primary target of this compound Hs Antagonist 7.8 – 8.0 pKi 79,118,120
⤷ pKi 7.9 – 8.0 [79,118]
pKi 7.8 [120]
cinnarizine Small molecule or natural product Approved drug Ligand has a PDB structure Rn Antagonist 7.9 pKi 58
⤷ pKi 7.9 (Ki 1.32x10-8 M) [58]
flunarizine Small molecule or natural product Approved drug Rn Antagonist 6.9 – 8.4 pKi 4,58
⤷ pKi 6.9 – 8.4 (Ki 1.12x10-7 – 3.96x10-9 M) [4,58]
pimozide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 7.6 pKi 120
⤷ pKi 7.6 [120]
sulpiride Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 7.2 – 7.9 pKi 25
⤷ pKi 7.2 – 7.9 (Ki 6x10-8 – 1.2x10-8 M) [25]
metoclopramide Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Mm Antagonist 7.5 pKi 81
⤷ pKi 7.5 (Ki 2.88x10-8 M) [81]
chlorpromazine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 7.5 pKi 120
⤷ pKi 7.5 [120]
lumateperone Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.5 pKi 73,117
⤷ pKi 7.5 (Ki 3.2x10-8 M) [73,117]
chlorpromazine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.0 – 7.6 pKi 41,118
⤷ pKi 7.0 – 7.6 [41,118]
quetiapine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 7.2 pKi 11
⤷ pKi 7.2 (Ki 6.9x10-8 M) [11]
(-)-sulpiride Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.3 – 8.0 pKi 41,118,125
⤷ pKi 6.3 – 8.0 (Ki 5.2x10-7 – 1x10-8 M) [41,118,125]
R-VK4-40 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.1 pKi 57
⤷ pKi 7.1 (Ki 7.58x10-8 M) [57]
(+)-sulpiride Small molecule or natural product Click here for species-specific activity table Rn Antagonist 7.0 pKi 120
⤷ pKi 7.0 [120]
ML321 Small molecule or natural product Primary target of this compound Hs Antagonist 7.0 pKi 135-136
⤷ pKi 7.0 (Ki 1x10-7 M) [135-136]
trans-flupenthixol Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.9 pKi 41
⤷ pKi 6.9 (Ki 1.2x10-7 M) [41]
EGIS-11150 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.9 pKi 42
⤷ pKi 6.9 (Ki 1.2x10-7 M) [42]
(+)-UH232 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.4 – 7.1 pKi 41,120
⤷ pKi 6.4 – 7.1 [41,120]
promazine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.5 pKi 26
⤷ pKi 6.5 (Ki 3x10-7 M) [26]
(+)-UH232 Small molecule or natural product Click here for species-specific activity table Rn Antagonist 6.4 pKi 120
⤷ pKi 6.4 [120]
clozapine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 5.8 – 6.9 pKi 41,75,114,118,125
⤷ pKi 5.8 – 6.9 [41,75,114,118,125]
clozapine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 6.2 pKi 120
⤷ pKi 6.2 [120]
(+)-S-14297 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.5 pKi 87
⤷ pKi 5.5 [87]
(+)-SCH-23390 Small molecule or natural product Hs Antagonist 5.3 pKi 41
⤷ pKi 5.3 [41]
iloperidone Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 7.0 pIC50 123
⤷ pIC50 7.0 (IC50 1.1x10-7 M) [123]
Description: Measuring displacement of [3H]spiperone from rat striatum.
metopimazine Small molecule or natural product Approved drug N/A Antagonist - -
⤷